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TW201945344A - 1-(5-substituted imidazol-1-yl)but-3-en derivatives and their use as fungicides - Google Patents

1-(5-substituted imidazol-1-yl)but-3-en derivatives and their use as fungicides Download PDF

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TW201945344A
TW201945344A TW108105389A TW108105389A TW201945344A TW 201945344 A TW201945344 A TW 201945344A TW 108105389 A TW108105389 A TW 108105389A TW 108105389 A TW108105389 A TW 108105389A TW 201945344 A TW201945344 A TW 201945344A
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alkyl
cycloalkyl
halogen
methyl
haloalkyl
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TW108105389A
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羅伯特 偉伯斯特
安德里亞斯 戈爾茨
路思 邁斯納
西比爾 拉普列希特
瑞查德 邁爾
大衛 伯尼爾
皮耶爾 伊芙 克庫爾朗恩
皮耶爾 金恩斯
史蒂芬尼 布魯尼特
菲利普 肯尼爾
多明尼克 拉奎爾
凡斯 托馬斯
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德商拜耳廠股份有限公司
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/66—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D233/90—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • A—HUMAN NECESSITIES
    • A01—AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
    • A01N—PRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
    • A01N43/00—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds
    • A01N43/48—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with two nitrogen atoms as the only ring hetero atoms
    • A01N43/56—1,2-Diazoles; Hydrogenated 1,2-diazoles
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/66—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D233/68—Halogen atoms

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Dentistry (AREA)
  • Pest Control & Pesticides (AREA)
  • Plant Pathology (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Agronomy & Crop Science (AREA)
  • General Health & Medical Sciences (AREA)
  • Wood Science & Technology (AREA)
  • Zoology (AREA)
  • Environmental Sciences (AREA)
  • Agricultural Chemicals And Associated Chemicals (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

The present invention relates to compounds of formula (I) wherein Q represents a 6-membered aromatic cycle as defined in the specification, and R1, R2, R3, R4, and R5 are defined as disclosed in the specification, to compositions comprising such compounds, and to the use of said compounds, in particular as fungicides.

Description

1-(5-取代的咪唑-1-基)丁-3-烯衍生物及其作為殺真菌劑之用途    1- (5-substituted imidazol-1-yl) but-3-ene derivatives and uses thereof as fungicides   

本發明係關於新穎的1-(5-取代的咪唑-1-基)丁-3-烯衍生物，較佳1-(5-取代的咪唑-1-基)丁-3-烯-2-醇、製備這些化合物的方法、包含這些之組成物、以及其作為生物活性化合物和組成物之用途，特別是用於作物保護和物料保護中防治有害的微生物。 The present invention relates to novel 1- (5-substituted imidazol-1-yl) but-3-ene derivatives, preferably 1- (5-substituted imidazol-1-yl) but-3-ene-2- Alcohols, methods for preparing these compounds, compositions containing these, and their use as biologically active compounds and compositions, especially for controlling harmful microorganisms in crop protection and material protection.

從WO 2016/156290 A1中已知，特定的1-(5-取代的咪唑-1-基)丙-2-醇衍生物和其鹽類顯示對抗廣譜的植物病原性真菌之良好殺真菌效用，且因此，為用於作物保護之有價值化合物。 It is known from WO 2016/156290 A1 that specific 1- (5-substituted imidazol-1-yl) propan-2-ol derivatives and salts thereof show good fungicidal efficacy against a broad spectrum of phytopathogenic fungi And, therefore, valuable compounds for crop protection.

然而，因為生態和經濟上對現代活性成份，例如殺真菌劑的要求持續增加，例如有關抗菌效譜、毒性、選擇性、施用率、殘留物的形成和有利製造，且亦可能有，例如抗藥性之問題，所以對於開發至少在某些領域具有優於已知的化合物和組成物之優點的新穎殺真菌化合物和組成物有持續的需求。 However, as ecological and economic requirements for modern active ingredients, such as fungicides, continue to increase, such as with regard to antimicrobial efficacy spectrum, toxicity, selectivity, application rates, formation of residues and favorable manufacturing, and there may also be, for example, There is a continuing need for the development of novel fungicidal compounds and compositions that have advantages over known compounds and compositions, at least in some areas.

因此，本發明之目標係藉由提供可用於作物保護和物料保護中防治有害的微生物之新穎化合物，特別是顯現殺真菌效用的化合物，來供給此需求。 Accordingly, the object of the present invention is to meet this need by providing novel compounds that can be used to control harmful microorganisms in crop protection and material protection, particularly compounds that exhibit fungicidal effects.

令人驚訝地，已發現特定的1-(5-取代的咪唑-1-基)丁-3-烯衍生物為有價值的殺真菌劑。 Surprisingly, specific 1- (5-substituted imidazol-1-yl) but-3-ene derivatives have been found to be valuable fungicides.

因此，本發明之目標為式(I)之化合物

Figure TW201945344A_D0001
其中R1 係代表氫、C1-C8-烷基、C2-C8-烯基、C2-C8-炔基、C3-C8-環烷基、C3-C8-環烷基-C1-C4-烷基、C1-C8-烷氧基、C1-C8-烷硫基、C6-C14-芳基、C6-C14-芳基-C1-C4-烷基、C6-C14-芳基-C2-C4-烯基或C6-C14-芳基-C2-C4-炔基，其中該R1之脂肪族部分，不包括環烷基部分，可帶有1、2、3或至多最大可能數目之相同或不同的Ra基團，其彼此獨立地係選自鹵素、CN、硝基、C1-C4-烷氧基和C1-C4-鹵基烷氧基，及其中R1的環烷基及/或芳基部分可帶有1、2、3、4、5或至多最大可能數目之相同或不同的Rb基團，其彼此獨立地係選自鹵素、CN、硝基、C1-C4-烷基、C1-C4-烷氧基、C1-C4-鹵烷基和C1-C4-鹵基烷氧基；R2 係代表氫、鹵素、氰基或-OR2a，其中R2a 係代表氫、C1-C8-烷基、-Si(R6a)(R6b)(R6c)、-P(O)(OH)2、-CH2-O-P(O)(OH)2、-C(O)-C1-C8-烷基、-C(O)-C3-C7-環烷基、-C(O)NH-C1-C8-烷基、-C(O)N-二-C1-C8-烷基或-C(O)O-C1-C8-烷基，其中-C(O)-C1-C8-烷基、-C(O)-C3-C7-環烷基、-C(O)NH-C1-C8-烷基、-C(O)N-二-C1-C8-烷基和-C(O)O-C1-C8-烷基為未經取代或經一或多個選自鹵素和C1-C8-烷氧基的基團取代，其中R6a、R6b、R6c相互獨立地係代表苯基或C1-C8-烷基； R3 係代表鹵素、羥基、氰基、異氰基、胺基、氫硫基(sulfanyl)、五氟-λ6-氫硫基、羧醛、羥基羰基、C2-C8-烷基、C1-C8-鹵烷基、C1-C8-氰基烷基、C1-C8-烷基氧基、C1-C8-鹵烷基氧基、三(C1-C8-烷基)矽基、三(C1-C8-烷基)矽基-C1-C8-烷基、C3-C7-環烷基、C3-C7-鹵基環烷基、C3-C7-環烯基、C3-C7-鹵基環烯基、C4-C10-環烷基烷基、C4-C10-鹵基環烷基烷基、C6-C12-環烷基環烷基、C1-C8-烷基-C3-C7-環烷基、C1-C8-烷氧基-C3-C7-環烷基、三(C1-C8-烷基)矽基-C3-C7-環烷基、C2-C8-烯基、C2-C8-炔基、C2-C8-烯基氧基、C2-C8-鹵基烯基氧基、C3-C8-炔基氧基、C3-C8-鹵基炔基氧基、C1-C8-烷基胺基、C1-C8-鹵烷基胺基、C1-C8-氰基烷氧基、C4-C8-環烷基烷氧基、C3-C6-環烷氧基、C1-C8-烷基氫硫基、C1-C8-鹵烷基氫硫基、C1-C8-烷基羰基、C1-C8-鹵烷基羰基、芳基羰基、芳基-C1-C6-烷基羰基、C3-C8-環烷基羰基、C3-C8-鹵基環烷基羰基、胺甲醯基、C1-C8-烷基胺甲醯基、二-C1-C8-烷基胺甲醯基、N-C1-C8-烷基氧基胺甲醯基、C1-C8-烷氧基胺甲醯基、N-C1-C8-烷基-C1-C8-烷氧基胺甲醯基、胺基硫羰基、C1-C8-烷氧基羰基、C1-C8-鹵基烷氧基羰基、C3-C8-環烷氧基羰基、C2-C8-烷氧基烷基羰基、C2-C8-鹵基烷氧基烷基羰基、C3-C10-環烷氧基烷基羰基、C1-C8-烷基胺基羰基、二-C1-C8-烷基胺基羰基、C3-C8-環烷基胺基羰基、C1-C8-烷基羰基氧基、C1-C8-鹵烷基羰基氧基、C3-C8-環烷基羰基氧基、C1-C8-烷基羰基胺基、C1-C8-鹵烷基羰基胺基、C1-C8-烷基胺基羰基氧基、二-C1-C8-烷基胺基羰基氧基、C1-C8-烷基氧基羰基氧基、C1-C8-烷基亞磺醯基、C1-C8-鹵烷基亞磺醯基、C1-C8-烷基磺醯基、C1-C8-鹵烷基磺醯基、C1-C8-烷基磺醯基氧基、C1-C8-鹵烷基磺醯基氧基、C1-C8-烷基胺基胺磺醯基(C1-C8-alkylaminosulfamoyl)、二-C1-C8-烷基胺基胺磺醯基、(C1-C8-烷氧基亞胺基)-C1-C8-烷基、(C3-C7-環烷氧基亞胺基)-C1-C8-烷基、羥基亞胺基-C1-C8-烷基、(C1-C8-烷氧基亞胺基)-C3-C7-環烷基、羥基亞胺基-C3-C7-環烷基、(C1-C8-烷基亞胺基)-氧基、(C1-C8-烷基亞胺基)-氧基-C1-C8-烷基、(C3-C7-環烷基亞胺基)-氧基-C1-C8-烷基、(C1-C6-烷基亞胺基)-氧基-C3-C7-環烷基、(C1-C8-烯基氧基 亞胺基)-C1-C8-烷基、(C1-C8-炔基氧基亞胺基)-C1-C8-烷基、(苯甲氧基亞胺基)-C1-C8-烷基、C1-C8-烷氧基烷基、C1-C8-烷硫基烷基、C1-C8-烷氧基烷氧基烷基、C1-C8-鹵基烷氧基烷基、苯甲基、苯基、5-員雜芳基、6-員雜芳基、苯甲氧基、苯氧基、苯甲基氫硫基、苯甲基胺基、苯基氫硫基或苯基胺基，其中苯甲基、苯基、5-員雜芳基、6-員雜芳基、苯甲氧基或苯氧基為未經取代或經一或多個選自下列之基團取代：鹵素、羥基、氰基、異氰基、胺基、氫硫基、五氟-λ6-氫硫基、羧醛、羥基羰基、C1-C8-烷基、C1-C8-鹵烷基、C1-C8-氰基烷基、C1-C8-烷基氧基、C1-C8-鹵烷基氧基、三(C1-C8-烷基)矽基、三(C1-C8-烷基)矽基-C1-C8-烷基、C3-C7-環烷基、C3-C7-鹵基環烷基、C3-C7-環烯基、C3-C7-鹵基環烯基、C4-C10-環烷基烷基、C4-C10-鹵基環烷基烷基、C6-C12-環烷基環烷基、C1-C8-烷基-C3-C7-環烷基、C1-C8-烷氧基-C3-C7-環烷基、三(C1-C8-烷基)矽基-C3-C7-環烷基、C2-C8-烯基、C2-C8-炔基、C2-C8-烯基氧基、C2-C8-鹵基烯基氧基、C3-C8-炔基氧基、C3-C8-鹵基炔基氧基、C1-C8-烷基胺基、C1-C8-鹵烷基胺基、C1-C8-氰基烷氧基、C4-C8-環烷基烷氧基、C3-C6-環烷氧基、C1-C8-烷基氫硫基、C1-C8-鹵烷基氫硫基、C1-C8-烷基羰基、C1-C8-鹵烷基羰基、芳基羰基、芳基-C1-C6-烷基羰基、C3-C8-環烷基羰基、C3-C8-鹵基環烷基羰基、C1-C8-烷基胺甲醯基、二-C1-C8-烷基胺甲醯基、N-C1-C8-烷基氧基胺甲醯基、C1-C8-烷氧基胺甲醯基、N-C1-C8-烷基-C1-C8-烷氧基胺甲醯基、胺基硫羰基、C1-C8-烷氧基羰基、C1-C8-鹵基烷氧基羰基、C3-C8-環烷氧基羰基、C2-C8-烷氧基烷基羰基、C2-C8-鹵基烷氧基烷基羰基、C3-C10-環烷氧基烷基羰基、C1-C8-烷基胺基羰基、二-C1-C8-烷基胺基羰基、C3-C8-環烷基胺基羰基、C1-C8-烷基羰基氧基、C1-C8-鹵烷基羰基氧基、C3-C8-環烷基羰基氧基、C1-C8-烷基羰基胺基、C1-C8-鹵烷基羰基胺基、C1-C8-烷基胺基羰基氧基、二-C1-C8-烷基胺基羰基氧基、C1-C8-烷基氧基羰基氧基、C1-C8-烷基亞磺醯基、C1-C8-鹵烷基亞磺醯基、C1-C8-烷基磺醯基、C1-C8-鹵烷基磺醯基、C1-C8-烷基磺醯基氧基、C1-C8-鹵烷基磺醯基氧基、C1-C8-烷基胺基胺磺醯基、二 -C1-C8-烷基胺基胺磺醯基、(C1-C8-烷氧基亞胺基)-C1-C8-烷基、(C3-C7-環烷氧基亞胺基)-C1-C8-烷基、羥基亞胺基-C1-C8-烷基、(C1-C8-烷氧基亞胺基)-C3-C7-環烷基、羥基亞胺基-C3-C7-環烷基、(C1-C8-烷基亞胺基)-氧基、(C1-C8-烷基亞胺基)-氧基-C1-C8-烷基、(C3-C7-環烷基亞胺基)-氧基-C1-C8-烷基、(C1-C6-烷基亞胺基)-氧基-C3-C7-環烷基、(C1-C8-烯基氧基亞胺基)-C1-C8-烷基、(C1-C8-炔基氧基亞胺基)-C1-C8-烷基、(苯甲氧基亞胺基)-C1-C8-烷基、C1-C8-烷氧基烷基、C1-C8-烷硫基烷基、C1-C8-烷氧基烷氧基烷基、C1-C8-鹵基烷氧基烷基、苯甲基、苯基、5-員雜芳基、6-員雜芳基、苯甲氧基、苯氧基、苯甲基氫硫基、苯甲基胺基、苯基氫硫基，或苯基胺基；R4 係代表氫、鹵素、C1-C8-烷基、C1-C8-鹵烷基、C1-C8-烷氧基、C1-C8-鹵基烷氧基、C1-C8-烷硫基或C1-C8-鹵基烷硫基；R5 係代表氫、鹵素、C1-C8-烷基、C1-C8-鹵烷基、C1-C8-烷氧基、C1-C8-鹵基烷氧基、C1-C8-烷硫基或C1-C8-鹵基烷硫基；及Q 係代表式(Q-I)之6-員芳香環
Figure TW201945344A_D0002
 其中U1 係代表CX1或N；U2 係代表CX2或N；U3 係代表CX3或N；U4 係代表CX4或N；U5 係代表CX5或N；其中X1、X2、X3、X4和X5相互獨立地係代表氫、鹵素、硝基、氰基、氫硫基、五氟-λ6-氫硫基、C1-C8-烷基、具有1至5個鹵素原子之C1-C8-鹵烷基、C3-C8-環烷基、具有1至5個鹵素原子之C3-C8- 鹵基環烷基、C1-C8-鹵烷基-C3-C7-環烷基、C3-C7-環烯基、C2-C8-烯基、C2-C8-炔基、C6-C12-雙環烷基(bicycloalkyl)、C3-C8-環烷基-C2-C8-烯基、C3-C8-環烷基-C2-C8-炔基、C1-C8-烷氧基、具有1至5個鹵素原子之C1-C8-鹵基烷氧基、C1-C8-烷氧基羰基、C1-C8-鹵基烷氧基羰基、C1-C8-烷基次磺醯基(sulfenyl)、C2-C8-烯基氧基、C3-C8-炔基氧基、C3-C6-環烷氧基、C1-C8-烷基亞磺醯基、C1-C8-烷基-磺醯基、三(C1-C8-烷基)-矽基氧基、三(C1-C8-烷基)-矽基、三(C1-C8-烷基)-矽基-C2-C8-炔基、三(C1-C8-烷基)-矽基-C2-C8-炔基氧基、C6-C14-芳基、C6-C14-芳基氧基、C6-C14-芳基次磺醯基、5-或6-員雜芳基、5-或6-員雜芳基氧基，其中C6-C14-芳基、C6-C14-芳基氧基、C6-C14-芳基次磺醯基、5-或6-員雜芳基、5-或6-員雜芳基氧基為未經取代或經一或多個選自下列之基團取代：鹵素、氰基氫硫基、五氟-λ6-氫硫基、C1-C8-烷基、C1-C8-鹵烷基、C1-C8-氰基烷基、C1-C8-烷基氧基、C1-C8-鹵烷基氧基、三(C1-C8-烷基)矽基、三(C1-C8-烷基)矽基-C1-C8-烷基、C3-C7-環烷基、C3-C7-鹵基環烷基、C3-C7-環烯基、C3-C7-鹵基環烯基、C4-C10-環烷基烷基、C4-C10-鹵基環烷基烷基、C6-C12-環烷基環烷基、C1-C8-烷基-C3-C7-環烷基、C1-C8-烷氧基-C3-C7-環烷基、三(C1-C8-烷基)矽基-C3-C7-環烷基、C2-C8-烯基、C2-C8-炔基、C2-C8-烯基氧基、C2-C8-鹵基烯基氧基、C3-C8-炔基氧基、C3-C8-鹵基炔基氧基、C1-C8-氰基烷氧基、C4-C8-環烷基烷氧基、C3-C6-環烷氧基、C1-C8-烷基氫硫基、C1-C8-鹵烷基氫硫基、C1-C8-烷基亞磺醯基、C1-C8-鹵烷基亞磺醯基、C1-C8-烷基磺醯基、C1-C8-鹵烷基磺醯基、C1-C8-烷基磺醯基氧基、C1-C8-鹵烷基磺醯基氧基、C1-C8-烷氧基烷基、C1-C8-烷硫基烷基、C1-C8-烷氧基烷氧基烷基、C1-C8-鹵基烷氧基烷基、苯甲基、苯基、5-員雜芳基、6-員雜芳基、6-員雜芳基氧基、苯甲氧基、苯氧基、苯甲基氫硫基和苯基氫硫基， 其中苯甲基、苯基、5-員雜芳基、6-員雜芳基、6-員雜芳基氧基、苯甲氧基、苯氧基、苯甲基氫硫基和苯基氫硫基為未經取代或經一或多個選自下列之基團取代：鹵素、CN、硝基、C1-C8-烷基、C1-C4-鹵烷基、C1-C4-烷氧基、C1-C4-鹵基烷氧基和五氟-λ6-氫硫基；且其中U1、U2、U3、U4和U5中最多二個係代表N；或U1和U2，或U2和U3，或U3和U4共同形成另外的飽和或不飽和的4至6-員經鹵素-或C1-C8-烷基取代或未經取代的環；及其鹽類和N-氧化物。 The object of the invention is therefore a compound of formula (I)
Figure TW201945344A_D0001
 Where R 1 represents hydrogen, C 1 -C 8 -alkyl, C 2 -C 8 -alkenyl, C 2 -C 8 -alkynyl, C 3 -C 8 -cycloalkyl, C 3 -C 8- Cycloalkyl-C 1 -C 4 -alkyl, C 1 -C 8 -alkoxy, C 1 -C 8 -alkylthio, C 6 -C 14 -aryl, C 6 -C 14 -aryl -C 1 -C 4 -alkyl, C 6 -C 14 -aryl-C 2 -C 4 -alkenyl or C 6 -C 14 -aryl-C 2 -C 4 -alkynyl, wherein the R 1 the aliphatic portion, excluding the cycloalkyl moiety, which may have three or up to the maximum possible number of identical or different groups R a, independently from each other selected from halogen, CN, nitro, C 1- C 4 -alkoxy and C 1 -C 4 -haloalkoxy, and the cycloalkyl and / or aryl portion of R 1 may carry 1, 2, 3, 4, 5 or up to a maximum Possible number of the same or different R b groups, which are independently selected from halogen, CN, nitro, C 1 -C 4 -alkyl, C 1 -C 4 -alkoxy, C 1 -C 4 -Haloalkyl and C 1 -C 4 -haloalkoxy; R 2 represents hydrogen, halogen, cyano or -OR 2a , where R 2a represents hydrogen, C 1 -C 8 -alkyl, -Si (R 6a) (R 6b) (R 6c), - P (O) (OH) 2, -CH 2 -OP (O) (OH) 2, -C (O) -C 1 -C 8 - alkoxy , -C (O) -C 3 -C 7 - cycloalkyl, -C (O) NH-C 1 -C 8 - alkyl, -C (O) N- two -C 1 -C 8 - alkyl Or -C (O) OC 1 -C 8 -alkyl, where -C (O) -C 1 -C 8 -alkyl, -C (O) -C 3 -C 7 -cycloalkyl, -C ( O) NH-C 1 -C 8 -alkyl, -C (O) N-di-C 1 -C 8 -alkyl and -C (O) OC 1 -C 8 -alkyl are unsubstituted or Substitution of one or more groups selected from halogen and C 1 -C 8 -alkoxy, wherein R 6a , R 6b , R 6c independently of one another represent phenyl or C 1 -C 8 -alkyl; R 3 Represents halogen, hydroxy, cyano, isocyano, amine, sulfanyl, pentafluoro-λ 6 -hydrothio, carboxaldehyde, hydroxycarbonyl, C 2 -C 8 -alkyl, C 1 -C 8 -haloalkyl, C 1 -C 8 -cyanoalkyl, C 1 -C 8 -alkyloxy, C 1 -C 8 -haloalkyloxy, tri (C 1 -C 8- Alkyl) silyl, tri (C 1 -C 8 -alkyl) silyl-C 1 -C 8 -alkyl, C 3 -C 7 -cycloalkyl, C 3 -C 7 -halocycloalkyl , C 3 -C 7 -cycloalkenyl, C 3 -C 7 -halocycloalkenyl, C 4 -C 10 -cycloalkylalkyl, C 4 -C 10 -halocycloalkylalkyl, C 6 -C 12 -cycloalkylcycloalkyl, C 1 -C 8 -alkyl-C 3 -C 7 -cycloalkyl, C 1 -C 8 -alkoxy-C 3 -C 7 -cycloalkyl, tri (C 1 -C 8 -alkyl) silyl-C 3 -C 7 -cycloalkyl, C 2 -C 8 -alkenyl, C 2 -C 8 -alkynyl , C 2 -C 8 -alkenyloxy, C 2 -C 8 -haloalkenyloxy, C 3 -C 8 -alkynyloxy, C 3 -C 8 -haloalkynyloxy, C 1 -C 8 -alkylamino, C 1 -C 8 -haloalkylamino, C 1 -C 8 -cyanoalkoxy, C 4 -C 8 -cycloalkylalkoxy, C 3- C 6 -cycloalkoxy, C 1 -C 8 -alkylhydrothio, C 1 -C 8 -haloalkylhydrothio, C 1 -C 8 -alkylcarbonyl, C 1 -C 8 -halo Alkylcarbonyl, arylcarbonyl, aryl-C 1 -C 6 -alkylcarbonyl, C 3 -C 8 -cycloalkylcarbonyl, C 3 -C 8 -halocycloalkylcarbonyl, carbamate, C 1 -C 8 -alkylamine formamyl, di-C 1 -C 8 -alkylamine formamyl, NC 1 -C 8 -alkyloxyamine formamyl, C 1 -C 8 -alkane Oxyamine formamyl, NC 1 -C 8 -alkyl-C 1 -C 8 -alkoxyamine formamyl, aminothiocarbonyl, C 1 -C 8 -alkoxycarbonyl, C 1 -C 8 -haloalkoxycarbonyl, C 3 -C 8 -cycloalkoxycarbonyl, C 2 -C 8 -alkoxyalkylcarbonyl, C 2 -C 8 -haloalkoxyalkylcarbonyl, C 3 -C 10 -cycloalkoxyalkylcarbonyl , C 1 -C 8 -alkylaminocarbonyl, di-C 1 -C 8 -alkylaminocarbonyl, C 3 -C 8 -cycloalkylaminocarbonyl, C 1 -C 8 -alkylcarbonyl Oxy, C 1 -C 8 -haloalkylcarbonyloxy, C 3 -C 8 -cycloalkylcarbonyloxy, C 1 -C 8 -alkylcarbonylamino, C 1 -C 8 -haloalkyl Carbonylamino, C 1 -C 8 -alkylaminocarbonyloxy, di-C 1 -C 8 -alkylaminocarbonyloxy, C 1 -C 8 -alkyloxycarbonyloxy, C 1 -C 8 -alkylsulfinylsulfenyl, C 1 -C 8 -haloalkylsulfinylsulfenyl, C 1 -C 8 -alkylsulfinylsulfenyl, C 1 -C 8 -haloalkylsulfinyl, C 1 -C 8 -alkylsulfonyloxy, C 1 -C 8 -haloalkylsulfonyloxy, C 1 -C 8 -alkylaminoaminesulfonyl (C 1 -C 8- alkylaminosulfamoyl), di-C 1 -C 8 -alkylaminoaminesulfonyl, (C 1 -C 8 -alkoxyimino) -C 1 -C 8 -alkyl, (C 3 -C 7 -Cycloalkoxyimino) -C 1 -C 8 -alkyl, hydroxyimino-C 1 -C 8 -alkyl, (C 1 -C 8 -alkoxyimino) -C 3 -C 7 -cycloalkyl, hydroxyimino-C 3 -C 7 -cycloalkyl, (C 1 -C 8 -alkylimino) -oxy, (C 1 -C 8 -alkylimine Amine) -oxy-C 1 -C 8- Alkyl, (C 3 -C 7 -cycloalkylimino) -oxy-C 1 -C 8 -alkyl, (C 1 -C 6 -alkylimino) -oxy-C 3- C 7 -cycloalkyl, (C 1 -C 8 -alkenyloxyimino) -C 1 -C 8 -alkyl, (C 1 -C 8 -alkynyloxyimino) -C 1 -C 8 -alkyl, (benzyloxyimino) -C 1 -C 8 -alkyl, C 1 -C 8 -alkoxyalkyl, C 1 -C 8 -alkylthioalkyl, C 1 -C 8 -alkoxyalkoxyalkyl, C 1 -C 8 -haloalkoxyalkyl, benzyl, phenyl, 5-membered heteroaryl, 6-membered heteroaryl, Benzyloxy, phenoxy, benzylhydrothio, benzylamino, phenylhydrothio or phenylamino, of which benzyl, phenyl, 5-membered heteroaryl, 6- Heteroaryl, benzyloxy or phenoxy is unsubstituted or substituted with one or more groups selected from the group consisting of: halogen, hydroxyl, cyano, isocyano, amine, hydrogenthio, penta Fluoro-λ 6 -hydrothio, carboxaldehyde, hydroxycarbonyl, C 1 -C 8 -alkyl, C 1 -C 8 -haloalkyl, C 1 -C 8 -cyanoalkyl, C 1 -C 8 - alkyloxy, C 1 -C 8 - haloalkyl group, tri (C 1 -C 8 - alkyl) of silicon-based, tri (C 1 -C 8 - alkyl) -C 1 -C silicon based 8 -alkane Group, C 3 -C 7 -cycloalkyl, C 3 -C 7 -halocycloalkyl, C 3 -C 7 -cycloalkenyl, C 3 -C 7 -halocycloalkenyl, C 4 -C 10 -cycloalkylalkyl, C 4 -C 10 -halocycloalkylalkyl, C 6 -C 12 -cycloalkylcycloalkyl, C 1 -C 8 -alkyl-C 3 -C 7- Cycloalkyl, C 1 -C 8 -alkoxy-C 3 -C 7 -cycloalkyl, tris (C 1 -C 8 -alkyl) silyl-C 3 -C 7 -cycloalkyl, C 2 -C 8 -alkenyl, C 2 -C 8 -alkynyl, C 2 -C 8 -alkenyloxy, C 2 -C 8 -haloalkenyloxy, C 3 -C 8 -alkynyloxy , C 3 -C 8 -haloalkynyloxy, C 1 -C 8 -alkylamino, C 1 -C 8 -haloalkylamino, C 1 -C 8 -cyanoalkoxy, C 4 -C 8 -cycloalkylalkoxy, C 3 -C 6 -cycloalkoxy, C 1 -C 8 -alkylhydrothio, C 1 -C 8 -haloalkylhydrothio, C 1 -C 8 -alkylcarbonyl, C 1 -C 8 -haloalkylcarbonyl, arylcarbonyl, aryl-C 1 -C 6 -alkylcarbonyl, C 3 -C 8 -cycloalkylcarbonyl, C 3- C 8 -halocycloalkylcarbonyl, C 1 -C 8 -alkylaminomethyl, di-C 1 -C 8 -alkylaminomethyl, NC 1 -C 8 -alkyloxyamine Fluorenyl, C 1 -C 8 -alkoxyamine methylamyl, NC 1 -C 8 -alkyl-C 1 -C 8 -Alkoxyaminomethane, aminothiocarbonyl, C 1 -C 8 -alkoxycarbonyl, C 1 -C 8 -haloalkoxycarbonyl, C 3 -C 8 -cycloalkoxy Carbonyl, C 2 -C 8 -alkoxyalkylcarbonyl, C 2 -C 8 -haloalkoxyalkylcarbonyl, C 3 -C 10 -cycloalkoxyalkylcarbonyl, C 1 -C 8 -Alkylaminocarbonyl, di-C 1 -C 8 -alkylaminocarbonyl, C 3 -C 8 -cycloalkylaminocarbonyl, C 1 -C 8 -alkylcarbonyloxy, C 1 -C 8 -haloalkylcarbonyloxy, C 3 -C 8 -cycloalkylcarbonyloxy, C 1 -C 8 -alkylcarbonylamino, C 1 -C 8 -haloalkylcarbonylamino, C 1- C 8 -alkylaminocarbonyloxy, di-C 1 -C 8 -alkylaminocarbonyloxy, C 1 -C 8 -alkyloxycarbonyloxy, C 1 -C 8 -alkylene Sulfonyl, C 1 -C 8 -haloalkylsulfinyl sulfenyl, C 1 -C 8 -alkylsulfonyl sulfenyl, C 1 -C 8 -haloalkylsulfonyl, C 1 -C 8 -alkane Sulfofluorenyloxy, C 1 -C 8 -haloalkylsulfonyloxy, C 1 -C 8 -alkylaminoaminesulfonyl, di-C 1 -C 8 -alkylaminoamine Sulfonyl, (C 1 -C 8 -alkoxyimino) -C 1 -C 8 -alkyl, (C 3 -C 7 -cycloalkoxyimino) -C 1 -C 8- Alkyl, hydroxyimino-C 1 -C 8 -alkyl, (C 1 -C 8 -alkoxyimino) -C 3 -C 7 -cycloalkyl, hydroxyimino-C 3- C 7 -cycloalkyl, (C 1 -C 8 -alkylimino) -oxy, (C 1 -C 8 -alkylimino) -oxy-C 1 -C 8 -alkyl, (C 3 -C 7 -cycloalkylimino) -oxy-C 1 -C 8 -alkyl, (C 1 -C 6 -alkylimino) -oxy-C 3 -C 7- Cycloalkyl, (C 1 -C 8 -alkenyloxyimino) -C 1 -C 8 -alkyl, (C 1 -C 8 -alkynyloxyimino) -C 1 -C 8 -Alkyl, (benzyloxyimino) -C 1 -C 8 -alkyl, C 1 -C 8 -alkoxyalkyl, C 1 -C 8 -alkylthioalkyl, C 1- C 8 -alkoxyalkoxyalkyl, C 1 -C 8 -haloalkoxyalkyl, benzyl, phenyl, 5-membered heteroaryl, 6-membered heteroaryl, benzyloxy Group, phenoxy, benzylhydrothio, benzylamino, phenylhydrothio, or phenylamino; R 4 represents hydrogen, halogen, C 1 -C 8 -alkyl, C 1 -C 8 -haloalkyl, C 1 -C 8 -alkoxy, C 1 -C 8 -haloalkoxy, C 1 -C 8 -alkylthio, or C 1 -C 8 -haloalkylthio R 5 represents hydrogen, halogen, C 1 -C 8 -alkyl, C 1 -C 8 -halogen Alkyl, C 1 -C 8 -alkoxy, C 1 -C 8 -haloalkoxy, C 1 -C 8 -alkylthio, or C 1 -C 8 -haloalkylthio; and the Q series 6-membered aromatic ring of representative formula (QI)
Figure TW201945344A_D0002
 Where U 1 represents CX 1 or N; U 2 represents CX 2 or N; U 3 represents CX 3 or N; U 4 represents CX 4 or N; U 5 represents CX 5 or N; where X 1 , X 2 , X 3 , X 4 and X 5 independently of one another represent hydrogen, halogen, nitro, cyano, hydrogenthio, pentafluoro-λ 6 -hydrothio, C 1 -C 8 -alkyl, have 1-5 halogen atoms C 1 -C 8 - haloalkyl, C 3 -C 8 - cycloalkyl having 1-5 C atoms, halogen of 3 -C 8 - cycloalkyl, halo, C 1 - C 8 -haloalkyl-C 3 -C 7 -cycloalkyl, C 3 -C 7 -cycloalkenyl, C 2 -C 8 -alkenyl, C 2 -C 8 -alkynyl, C 6 -C 12 -Bicycloalkyl, C 3 -C 8 -cycloalkyl-C 2 -C 8 -alkenyl, C 3 -C 8 -cycloalkyl-C 2 -C 8 -alkynyl, C 1 -C 8 -alkoxy, C 1 -C 8 -haloalkoxy having 1 to 5 halogen atoms, C 1 -C 8 -alkoxycarbonyl, C 1 -C 8 -haloalkoxycarbonyl, C 1 -C 8 -alkylsulfenyl, C 2 -C 8 -alkenyloxy, C 3 -C 8 -alkynyloxy, C 3 -C 6 -cycloalkoxy, C 1 -C 8 -alkylsulfinamidino, C 1 -C 8 -alkyl-sulfofluorenyl, tris (C 1 -C 8 -alkyl) -silyloxy, tris (C 1 -C 8- Alkyl) -Si Tris (C 1 -C 8 -alkyl) -silyl-C 2 -C 8 -alkynyl, tris (C 1 -C 8 -alkyl) -silyl-C 2 -C 8 -alkynyloxy C 6 -C 14 -aryl, C 6 -C 14 -aryloxy, C 6 -C 14 -arylsulfenyl, 5- or 6-membered heteroaryl, 5- or 6- Heteroarylaryloxy, wherein C 6 -C 14 -aryl, C 6 -C 14 -aryloxy, C 6 -C 14 -arylsulfenylfluorenyl, 5- or 6-membered heteroaryl , 5- or 6-membered heteroaryloxy is unsubstituted or substituted with one or more groups selected from the group consisting of halogen, cyanohydrothio, pentafluoro-λ 6 -hydrothio, C 1 -C 8 -alkyl, C 1 -C 8 -haloalkyl, C 1 -C 8 -cyanoalkyl, C 1 -C 8 -alkyloxy, C 1 -C 8 -haloalkyloxy , Tris (C 1 -C 8 -alkyl) silyl, tris (C 1 -C 8 -alkyl) silyl-C 1 -C 8 -alkyl, C 3 -C 7 -cycloalkyl, C 3 -C 7 -halocycloalkyl, C 3 -C 7 -cycloalkenyl, C 3 -C 7 -halocycloalkenyl, C 4 -C 10 -cycloalkylalkyl, C 4 -C 10- Halocycloalkylalkyl, C 6 -C 12 -cycloalkylcycloalkyl, C 1 -C 8 -alkyl-C 3 -C 7 -cycloalkyl, C 1 -C 8 -alkoxy- C 3 -C 7 - cycloalkyl, tri (C 1 -C 8 - alkyl) silicon based -C 3 -C 7 - cycloalkyl , C 2 -C 8 - alkenyl, C 2 -C 8 - alkynyl, C 2 -C 8 - alkenyl group, C 2 -C 8 - alkenyl group having a halogen group, C 3 -C 8 - alkynyl Alkoxy, C 3 -C 8 -haloalkynyloxy, C 1 -C 8 -cyanoalkoxy, C 4 -C 8 -cycloalkylalkoxy, C 3 -C 6 -cycloalkane alkoxy, C 1 -C 8 - alkyl mercapto, C 1 -C 8 - haloalkyl group hydrogen, C 1 -C 8 - alkylsulfinyl acyl, C 1 -C 8 - haloalkyl Sulfinylene, C 1 -C 8 -alkylsulfonyl, C 1 -C 8 -haloalkylsulfonyl, C 1 -C 8 -alkylsulfonyloxy, C 1 -C 8- haloalkyl acyl group sulfo, C 1 -C 8 - alkoxyalkyl, C 1 -C 8 - alkylthio group, C 1 -C 8 - alkoxyalkoxy -alkyl, C 1 -C 8 -haloalkoxyalkyl, benzyl, phenyl, 5-membered heteroaryl, 6-membered heteroaryl, 6-membered heteroaryloxy, benzyloxy, phenoxy Benzylhydrothio and phenylhydrothio, among which benzyl, phenyl, 5-membered heteroaryl, 6-membered heteroaryl, 6-membered heteroaryloxy, benzyloxy, Phenoxy, benzylhydrothio, and phenylhydrothio are unsubstituted or substituted with one or more groups selected from the group consisting of: halogen, CN, nitro, C 1- C 8 -alkyl, C 1 -C 4 -haloalkyl, C 1 -C 4 -alkoxy, C 1 -C 4 -haloalkoxy, and pentafluoro-λ 6 -hydrothio group; And at most two of U 1 , U 2 , U 3 , U 4 and U 5 represent N; or U 1 and U 2 , or U 2 and U 3 , or U 3 and U 4 together form another saturation or unsaturated 4 to 6-membered halogen - or C 1 -C 8 - alkyl substituted or unsubstituted ring; and salts and N- oxides.

如式(Q-I)中之箭號，係描繪所示的部分與分子其餘部分的鍵結位置。 As shown by the arrow in formula (Q-I), it depicts the bonding position between the part shown and the rest of the molecule.

上文和下文所示的化學式之較佳基團定義係如下所示。這些定義適用於式(I)、(Ia)、(Ib)和(Ic)之最終產物及同樣適用於析出物和中間物。 The preferred group definitions of the chemical formulae shown above and below are shown below. These definitions apply to the final products of formulae (I), (Ia), (Ib) and (Ic) and also to the precipitates and intermediates.

R1 較佳地係代表C1-C8-烷基、C3-C8-環烷基、C6-C14-芳基或C6-C14-芳基-C1-C4-烷基，其中R1之脂肪族部分，不包括環烷基部分，可帶有1、2、3或至多最大可能數目之相同或不同的Ra基團，其彼此獨立地係選自鹵素、CN、硝基、C1-C4-烷氧基和C1-C4-鹵基烷氧基；及其中R1之環烷基及/或芳基部分可帶有1、2、3、4、5或至多最大數目之相同或不同的Rb基團，其彼此獨立地係選自鹵素、CN、硝基、C1-C4-烷基、C1-C4-烷氧基、C1-C4-鹵烷基和C1-C4-鹵基烷氧基。 R 1 preferably represents C 1 -C 8 -alkyl, C 3 -C 8 -cycloalkyl, C 6 -C 14 -aryl or C 6 -C 14 -aryl-C 1 -C 4- Alkyl, wherein the aliphatic portion of R 1 , excluding the cycloalkyl portion, may carry 1, 2, 3 or up to the maximum possible number of the same or different R a groups, which are independently selected from halogen, CN, nitro, C 1 -C 4 -alkoxy and C 1 -C 4 -haloalkoxy; and the cycloalkyl and / or aryl portion of R 1 may bear 1, 2, 3, 4, 5 or up to a maximum number of the same or different R b groups, which are independently of one another selected from halogen, CN, nitro, C 1 -C 4 -alkyl, C 1 -C 4 -alkoxy, C 1 -C 4 -haloalkyl and C 1 -C 4 -haloalkoxy.

R1 更佳地係代表C1-C8-烷基、C1-C8-鹵烷基、C3-C8-環烷基、C6-C14-芳基或C6-C14-芳基-C1-C4-烷基，其中R1的環烷基及/或芳基部分可帶有1或2個相同或不同的Rb基團，其彼此獨立地係選自鹵素、CN、硝基、C1-C4-烷基、C1-C4-烷氧基、C1-C4-鹵烷基和C1-C4-鹵基烷氧基。 R 1 more preferably represents C 1 -C 8 -alkyl, C 1 -C 8 -haloalkyl, C 3 -C 8 -cycloalkyl, C 6 -C 14 -aryl or C 6 -C 14 -Aryl-C 1 -C 4 -alkyl, wherein the cycloalkyl and / or aryl moiety of R 1 may carry 1 or 2 identical or different R b groups, which are independently selected from halogens , CN, nitro, C 1 -C 4 -alkyl, C 1 -C 4 -alkoxy, C 1 -C 4 -haloalkyl, and C 1 -C 4 -haloalkoxy.

R1 更佳地係代表視需要經鹵素-或C1-C4-烷基-取代的C3-C7-環烷基、視需要經鹵素-或C1-C4-烷基-取代的苯基或視需要經鹵素-或C1-C4-烷基-取代的苯甲基。 More preferably R 1 optionally halogen-based Representative - or C 1 -C 4 - alkyl - substituted C 3 -C 7 - cycloalkyl, optionally halogen - or C 1 -C 4 - alkyl - substituted or phenyl optionally halogen - or C 1 -C 4 - alkyl - substituted benzyl.

R1 更佳地係代表視需要經氟-、氯-、溴-、甲基-、乙基-、正丙基-、異丙基-、正丁基-、異丁基-或第三丁基-取代的C3-C6-環烷基，視需要經氟-、氯-、溴-、甲基-、乙基-、正丙基-、異丙基-、正丁基-、異丁基-或第三丁基-取代的苯基或視需要經氟-、氯-、溴-、甲基-、乙基-、正丙基-、異丙基-、正丁基-、異丁基-或第三丁基-取代的苯甲基。 R 1 more preferably represents fluorine-, chlorine-, bromine-, methyl-, ethyl-, n-propyl-, isopropyl-, n-butyl-, isobutyl- or tert-butyl as needed -Substituted C 3 -C 6 -cycloalkyl, optionally via fluorine-, chloro-, bromo-, methyl-, ethyl-, n-propyl-, isopropyl-, n-butyl-, iso- Butyl- or third-butyl-substituted phenyl or optionally fluorine-, chlorine-, bromine-, methyl-, ethyl-, n-propyl-, isopropyl-, n-butyl-, iso- Butyl- or tert-butyl-substituted benzyl.

R1 更佳地係代表視需要經氟-、氯-、溴-、甲基-、乙基-、正丙基-、異丙基-、正丁基-、異丁基-或第三丁基-取代的環丙基、視需要經氟-、氯-、溴-、甲基-、乙基-、正丙基-、異丙基-、正丁基-、異丁基-或第三丁基-取代的苯基或視需要經氟-、氯-、溴-、甲基-、乙基-、正丙基-、異丙基-、正丁基-、異丁基-或第三丁基-取代的苯甲基。 R 1 more preferably represents fluorine-, chlorine-, bromine-, methyl-, ethyl-, n-propyl-, isopropyl-, n-butyl-, isobutyl- or tert-butyl as needed -Substituted cyclopropyl, optionally fluorine-, chloro-, bromo-, methyl-, ethyl-, n-propyl-, isopropyl-, n-butyl-, isobutyl-, or tertiary Butyl-substituted phenyl or optionally fluorine-, chloro-, bromo-, methyl-, ethyl-, n-propyl-, isopropyl-, n-butyl-, isobutyl-, or tertiary Butyl-substituted benzyl.

R1 更佳地係代表環丙基、1-氟環丙基、1-氯環丙基、1-溴環丙基、1-甲基環丙基、1-乙基環丙基、視需要經氟-、氯-，或溴-取代的苯基或視需要經氟-、氯-或溴-取代的苯甲基。 R 1 more preferably represents cyclopropyl, 1-fluorocyclopropyl, 1-chlorocyclopropyl, 1-bromocyclopropyl, 1-methylcyclopropyl, 1-ethylcyclopropyl, as required Fluoro-, chloro-, or bromo-substituted phenyl or optionally fluoro-, chloro-, or bromo-substituted benzyl.

R1 更佳地係代表環丙基、1-氟環丙基、1-氯環丙基、1-溴環丙基、1-甲基環丙基、1-乙基環丙基、苯基、經氟-取代的苯基、苯甲基或經氟-取代的苯甲基。 R 1 more preferably represents cyclopropyl, 1-fluorocyclopropyl, 1-chlorocyclopropyl, 1-bromocyclopropyl, 1-methylcyclopropyl, 1-ethylcyclopropyl, phenyl , Fluorine-substituted phenyl, benzyl or fluorine-substituted benzyl.

R1 更佳地係代表環丙基、1-氟環丙基、1-氯環丙基、1-溴環丙基、1-甲基環丙基、1-乙基環丙基、苯基、2-氟苯基、3-氟苯基、4-氟苯基、2,3-二氟苯基、2,4-二氟苯基、2,5-二氟苯基、2,6-二氟苯基、2-氟-3-氯苯基、2-氟-4-氯苯基、2-氟-5-氯苯基、2-氟-6-氯苯基、2-氯-3-氟苯基、2-氯-4-氟苯基、2-氯-5-氟苯基或苯甲基。 R 1 more preferably represents cyclopropyl, 1-fluorocyclopropyl, 1-chlorocyclopropyl, 1-bromocyclopropyl, 1-methylcyclopropyl, 1-ethylcyclopropyl, phenyl , 2-fluorophenyl, 3-fluorophenyl, 4-fluorophenyl, 2,3-difluorophenyl, 2,4-difluorophenyl, 2,5-difluorophenyl, 2,6- Difluorophenyl, 2-fluoro-3-chlorophenyl, 2-fluoro-4-chlorophenyl, 2-fluoro-5-chlorophenyl, 2-fluoro-6-chlorophenyl, 2-chloro-3 -Fluorophenyl, 2-chloro-4-fluorophenyl, 2-chloro-5-fluorophenyl or benzyl.

R1 最佳地係代表1-氟環丙基、1-氯環丙基、2,4-二氟苯基、或苯甲基。 R 1 most preferably represents 1-fluorocyclopropyl, 1-chlorocyclopropyl, 2,4-difluorophenyl, or benzyl.

R2 較佳地係代表氫、氟、氯、氰基或-OR2a。 R 2 preferably represents hydrogen, fluorine, chlorine, cyano or -OR 2a .

R2 更佳地係代表-OR2a。 R 2 more preferably represents -OR 2a .

R2a 較佳地係代表H、C1-C8-烷基或經鹵素-或C1-C8-烷氧基-取代的或未經取代的-C(O)-C1-C8-烷基。 R 2a preferably represents H, C 1 -C 8 -alkyl or halogen- or C 1 -C 8 -alkoxy-substituted or unsubstituted -C (O) -C 1 -C 8 -alkyl.

R2a 更佳地係代表H或C1-C8-烷基。 R 2a more preferably represents H or C 1 -C 8 -alkyl.

R2a 更佳地係代表H、甲基、乙基、正丙基、異丙基、正丁基、異丁基或第三丁基。 R 2a more preferably represents H, methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl or third butyl.

R2a 最佳地係代表H。 R 2a best represents H.

R2 最佳地係代表-OH。 R 2 best represents -OH.

R3 較佳地係代表鹵素、羥基、氰基、異氰基、硝基、羧醛、羥基羰基、C1-C8-烷基、C1-C8-鹵烷基、C1-C8-氰基烷基、C1-C8-烷基氧基、C1-C8-鹵烷基氧基、C3-C7-環烷基、C3-C7-鹵基環烷基、C2-C8-烯基、C2-C8-炔基、C2-C8-烯基氧基、C2-C8-鹵基烯基氧基、C3-C8-炔基氧基、C3-C8-鹵炔基氧基、C1-C8-烷基氫硫基、C1-C8-鹵烷基氫硫基、C1-C8-烷基羰基、C1-C8-鹵烷基羰基、C6-C14-芳基羰基、C6-C14-芳基-C1-C6-烷基羰基、C3-C8-環烷基羰基、C3-C8-鹵基環烷基羰基、胺基硫羰基、胺甲醯基、C1-C8-烷氧基羰基、C1-C8-鹵基烷氧基羰基、C3-C8-環烷氧基羰基、C1-C8-烷基羰基氧基、C1-C8-鹵烷基羰基氧基、C3-C8-環烷基羰基氧基、苯甲基、苯基、5-員雜芳基、6-員雜芳基、苯甲氧基或苯氧基，其中苯甲基、苯基、5-員雜芳基、6-員雜芳基、苯甲氧基和苯氧基視需要經一或多個選自下列之基團取代：鹵素、羥基、氰基、異氰基、胺基、氫硫基、五氟-λ6-氫硫基、C1-C8-烷基、C1-C8-鹵烷基、C1-C8-烷基氧基、C1-C8-鹵烷基氧基、三(C1-C8-烷基)矽基、C3-C7-環烷基、C2-C8-烯基和C2-C8-炔基。 R 3 preferably represents halogen, hydroxy, cyano, isocyano, nitro, carboxaldehyde, hydroxycarbonyl, C 1 -C 8 -alkyl, C 1 -C 8 -haloalkyl, C 1 -C 8 -cyanoalkyl, C 1 -C 8 -alkyloxy, C 1 -C 8 -haloalkyloxy, C 3 -C 7 -cycloalkyl, C 3 -C 7 -halocycloalkane , C 2 -C 8 -alkenyl, C 2 -C 8 -alkynyl, C 2 -C 8 -alkenyloxy, C 2 -C 8 -haloalkenyloxy, C 3 -C 8- Alkynyloxy, C 3 -C 8 -haloalkynyloxy, C 1 -C 8 -alkylhydrosulfanyl, C 1 -C 8 -haloalkylhydrosulfanyl, C 1 -C 8 -alkyl Carbonyl, C 1 -C 8 -haloalkylcarbonyl, C 6 -C 14 -arylcarbonyl, C 6 -C 14 -aryl-C 1 -C 6 -alkylcarbonyl, C 3 -C 8 -cycloalkane Carbonyl, C 3 -C 8 -halocycloalkylcarbonyl, aminothiocarbonyl, carbamoyl, C 1 -C 8 -alkoxycarbonyl, C 1 -C 8 -haloalkoxycarbonyl, C 3 -C 8 -cycloalkoxycarbonyl, C 1 -C 8 -alkylcarbonyloxy, C 1 -C 8 -haloalkylcarbonyloxy, C 3 -C 8 -cycloalkylcarbonyloxy, Benzyl, phenyl, 5-membered heteroaryl, 6-membered heteroaryl, benzyloxy or phenoxy, of which benzyl, phenyl, 5-membered heteroaryl , 6-membered heteroaryl, benzyloxy, and phenoxy are optionally substituted with one or more groups selected from the group consisting of halogen, hydroxyl, cyano, isocyano, amine, hydrogenthio, and Fluoro-λ 6 -hydrosulfanyl, C 1 -C 8 -alkyl, C 1 -C 8 -haloalkyl, C 1 -C 8 -alkyloxy, C 1 -C 8 -haloalkyloxy , Tris (C 1 -C 8 -alkyl) silyl, C 3 -C 7 -cycloalkyl, C 2 -C 8 -alkenyl and C 2 -C 8 -alkynyl.

R3 更佳地係代表鹵素、氰基、硝基、羧醛、羥基羰基、C1-C4-烷基、C1-C4-鹵烷基、C1-C4-氰基烷基、C1-C4-烷基氧基、C1-C4-鹵烷基氧基、C3-C6-環烷基、C3-C6-鹵基環烷基、C2-C4-烯基、C2-C4-炔基、C1-C4-烷基氫硫基、C1-C4-鹵烷基氫硫基、C1-C4-烷基羰基、C1-C4-鹵烷基羰基、胺基硫羰基、胺甲醯基、C1-C4-烷氧基羰基或C1-C4-鹵素基烷氧基羰基。 R 3 more preferably represents halogen, cyano, nitro, carboxaldehyde, hydroxycarbonyl, C 1 -C 4 -alkyl, C 1 -C 4 -haloalkyl, C 1 -C 4 -cyanoalkyl , C 1 -C 4 -alkyloxy, C 1 -C 4 -haloalkyloxy, C 3 -C 6 -cycloalkyl, C 3 -C 6 -halocycloalkyl, C 2 -C 4 -alkenyl, C 2 -C 4 -alkynyl, C 1 -C 4 -alkylhydrosulfanyl, C 1 -C 4 -haloalkylhydrosulfanyl, C 1 -C 4 -alkylcarbonyl, C 1- C 4 -haloalkylcarbonyl, aminothiocarbonyl, carbamate, C 1 -C 4 -alkoxycarbonyl or C 1 -C 4 -haloalkoxycarbonyl.

R3 更佳地係代表氟、氯、溴、碘、氰基、硝基、胺基硫羰基、C1-C4-鹵烷基或胺甲醯基。 R 3 more preferably represents fluorine, chlorine, bromine, iodine, cyano, nitro, aminothiocarbonyl, C 1 -C 4 -haloalkyl or carbamate.

R3 更佳地係代表氟、氯、溴、碘、氰基、胺基硫羰基或C1-C4-鹵烷基。 R 3 more preferably represents fluorine, chlorine, bromine, iodine, cyano, aminothiocarbonyl or C 1 -C 4 -haloalkyl.

R3 更佳地係代表氟、氯、溴、碘、氰基、胺基硫羰基、氯甲基、溴甲基、二氯甲基、三氯甲基、氟甲基、二氟甲基、三氟甲基、氯氟甲基、二氯氟甲基、氯二氟甲基、1-氯乙基、1-溴乙基、1-氟乙基、2-氟乙基、2,2-二氟乙基、2,2,2-三氟乙基、2-氯-2-氟乙基、2-氯-2,2-二氟乙基、2,2-二氯-2-氟乙基、2,2,2-三氯乙基、五氟乙基或1,1,1-三氟丙-2-基。 R 3 more preferably represents fluorine, chlorine, bromine, iodine, cyano, aminothiocarbonyl, chloromethyl, bromomethyl, dichloromethyl, trichloromethyl, fluoromethyl, difluoromethyl, Trifluoromethyl, chlorofluoromethyl, dichlorofluoromethyl, chlorodifluoromethyl, 1-chloroethyl, 1-bromoethyl, 1-fluoroethyl, 2-fluoroethyl, 2,2- Difluoroethyl, 2,2,2-trifluoroethyl, 2-chloro-2-fluoroethyl, 2-chloro-2,2-difluoroethyl, 2,2-dichloro-2-fluoroethyl Radical, 2,2,2-trichloroethyl, pentafluoroethyl or 1,1,1-trifluoroprop-2-yl.

R3 更佳地係代表氟、氰基或CF3。 R 3 more preferably represents fluorine, cyano or CF 3 .

R3 最佳地係代表氰基或CF3。 R 3 most preferably represents cyano or CF 3 .

R4 較佳地係代表氫、氟、甲基、乙基、正丙基、異丙基、正丁基、異丁基或第三丁基。 R 4 preferably represents hydrogen, fluorine, methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl or third butyl.

R4 更佳地係代表氫、氟、甲基或乙基。 R 4 more preferably represents hydrogen, fluorine, methyl or ethyl.

R4 更佳地係代表氫、氟或甲基。 R 4 more preferably represents hydrogen, fluorine or methyl.

R4 更佳地係代表氫或甲基。 R 4 more preferably represents hydrogen or methyl.

R5 較佳地係代表氫、氟、甲基、乙基、正丙基、異丙基、正丁基、異丁基或第三丁基。 R 5 preferably represents hydrogen, fluorine, methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl or third butyl.

R5 更佳地係代表氫、氟、甲基或乙基。 R 5 more preferably represents hydrogen, fluorine, methyl or ethyl.

R5 更佳地係代表氫、氟或甲基。 R 5 more preferably represents hydrogen, fluorine or methyl.

R5 更佳地係代表氫或甲基。 R 5 more preferably represents hydrogen or methyl.

最佳地至少R4和R5其中之一係代表氫而另一個係代表氫或甲基。 Most preferably at least one of R 4 and R 5 represents hydrogen and the other represents hydrogen or methyl.

Q 較佳地係代表含有一或二個氮原子之經取代6-員芳香雜環或經取代6-員芳香碳環。經取代係指特定化學式之環係包括至少X1、X2、X3、X4或X5中之一者不為氫。 Q preferably represents a substituted 6-membered aromatic heterocyclic ring or a substituted 6-membered aromatic carbocyclic ring containing one or two nitrogen atoms. Substituted means that a ring system of a specific chemical formula includes at least one of X 1 , X 2 , X 3 , X 4 or X 5 is not hydrogen.

Q 更佳地係代表較佳經取代之式(Q-I-1)至(Q-I-10)之6-員芳香環 Q is more preferably a 6-membered aromatic ring of the preferred substituted formulas (Q-I-1) to (Q-I-10)

Figure TW201945344A_D0003
Figure TW201945344A_D0003
Figure TW201945344A_D0004
Figure TW201945344A_D0004

其中X1、X2、X3、X4和X5具有如上述式(I)所給予之相同定義。較佳的X1、X2、X3、X4和X5之定義係如下所示。 Wherein X 1 , X 2 , X 3 , X 4 and X 5 have the same definitions as given by the above formula (I). The preferred definitions of X 1 , X 2 , X 3 , X 4 and X 5 are shown below.

Q 更佳地係代表較佳經取代的式(Q-I-1)至(Q-I-3)之苯基、3-吡啶基或4-吡啶基 Q more preferably represents phenyl, 3-pyridyl or 4-pyridyl of the preferred substituted formulae (Q-I-1) to (Q-I-3)

Figure TW201945344A_D0005
Figure TW201945344A_D0005

其中X1、X2、X3、X4和X5具有如上述式(I)所給予之相同定義。較佳的X1、X2、X3、X4和X5之定義係如下所示。 Wherein X 1 , X 2 , X 3 , X 4 and X 5 have the same definitions as given by the above formula (I). The preferred definitions of X 1 , X 2 , X 3 , X 4 and X 5 are shown below.

Q 更佳地係代表較佳經取代的式(Q-I-1)或(Q-I-2)之苯基或3-吡啶基 Q is more preferably a phenyl or 3-pyridyl group of the preferred substituted formula (Q-I-1) or (Q-I-2)

Figure TW201945344A_D0006
Figure TW201945344A_D0006

其中X1、X2、X3、X4和X5具有如上述式(I)所給予之相同定義。較佳的X1、X2、X3、X4和X5之定義係如下所示。 Wherein X 1 , X 2 , X 3 , X 4 and X 5 have the same definitions as given by the above formula (I). The preferred definitions of X 1 , X 2 , X 3 , X 4 and X 5 are shown below.

Q 最佳地係代表較佳經取代的式(Q-I-1)之苯基 Q is most preferably a phenyl group of the preferred substituted formula (Q-I-1)

Figure TW201945344A_D0007
Figure TW201945344A_D0007

其中X1、X2、X3、X4和X5具有如上述式(I)所給予之相同定義。較佳的X1、X2、X3、X4和X5之定義係如下所示。 Wherein X 1 , X 2 , X 3 , X 4 and X 5 have the same definitions as given by the above formula (I). The preferred definitions of X 1 , X 2 , X 3 , X 4 and X 5 are shown below.

X1、X2、X3、X4和X5相互獨立地較佳地係代表氫、鹵素、硝基、氰基、氫硫基、五氟-λ6-氫硫基、C1-C8-烷基、具有1至5個鹵素原子之C1-C8-鹵烷基、C3-C8-環烷基、具有1至5個鹵素原子之C3-C8-鹵基環烷基、 C1-C8-鹵烷基-C3-C7-環烷基、C3-C7-環烯基、C2-C8-烯基、C2-C8-炔基、C6-C12-雙環烷基、C3-C8-環烷基-C2-C8-烯基、C3-C8-環烷基-C2-C8-炔基、C1-C8-烷氧基、具有1至5個鹵素原子之C1-C8-鹵基烷氧基、C1-C8-烷氧基羰基、C1-C8-鹵基烷氧基羰基、C1-C8-烷基次磺醯基、C2-C8-烯基氧基、C3-C8-炔基氧基、C3-C6-環烷氧基、C1-C8-烷基亞磺醯基、C1-C8-烷基磺醯基、三(C1-C8-烷基)-矽基氧基、三(C1-C8-烷基)-矽基、三(C1-C8-烷基)-矽基-C2-C8-炔基、三(C1-C8-烷基)-矽基-C2-C8-炔基氧基、C6-C14-芳基、C6-C14-芳基氧基、C6-C14-芳基次磺醯基、5-或6-員雜芳基，或5-或6-員雜芳基氧基，其中C6-C14-芳基、C6-C14-芳基氧基、C6-C14-芳基次磺醯基、5-或6-員雜芳基和5-或6-員雜芳基氧基為未經取代或經一或多個選自下列之基團取代：鹵素、氰基氫硫基、五氟-λ6-氫硫基、C1-C8-烷基、C1-C8-鹵烷基、C1-C8-氰基烷基、C1-C8-烷基氧基、C1-C8-鹵烷基氧基、三(C1-C8-烷基)矽基、三(C1-C8-烷基)矽基-C1-C8-烷基、C3-C7-環烷基、C3-C7-鹵基環烷基、C3-C7-環烯基、C3-C7-鹵基環烯基、C4-C10-環烷基烷基、C4-C10-鹵基環烷基烷基、C6-C12-環烷基環烷基、C1-C8-烷基-C3-C7-環烷基、C1-C8-烷氧基-C3-C7-環烷基、三(C1-C8-烷基)矽基-C3-C7-環烷基、C2-C8-烯基、C2-C8-炔基、C2-C8-烯基氧基、C2-C8-鹵基烯基氧基、C3-C8-炔基氧基、C3-C8-鹵基炔基氧基、C1-C8-氰基烷氧基、C4-C8-環烷基烷氧基、C3-C6-環烷氧基、C1-C8-烷基氫硫基、C1-C8-鹵烷基氫硫基、C1-C8-烷基亞磺醯基、C1-C8-鹵烷基亞磺醯基、C1-C8-烷基磺醯基、C1-C8-鹵烷基磺醯基、C1-C8-烷基磺醯基氧基、C1-C8-鹵烷基磺醯基氧基、C1-C8-烷氧基烷基、C1-C8-烷硫基烷基、C1-C8-烷氧基烷氧基烷基、C1-C8-鹵基烷氧基烷基、苯甲基、苯基、5-員雜芳基、6-員雜芳基、6-員雜芳基氧基、苯甲氧基、苯氧基、苯甲基氫硫基和苯基氫硫基。 X 1 , X 2 , X 3 , X 4 and X 5 are preferably independently of each other hydrogen, halogen, nitro, cyano, hydrogenthio, pentafluoro-λ 6 -hydrothio, C 1 -C 8 - alkyl group having a C 1 to 5 halogen atoms 1 -C 8 - haloalkyl, C 3 -C 8 - cycloalkyl group having a C 1 to 5 halogen atoms 3 -C 8 - cycloalkyl halo Alkyl, C 1 -C 8 -haloalkyl-C 3 -C 7 -cycloalkyl, C 3 -C 7 -cycloalkenyl, C 2 -C 8 -alkenyl, C 2 -C 8 -alkynyl , C 6 -C 12 -bicycloalkyl, C 3 -C 8 -cycloalkyl-C 2 -C 8 -alkenyl, C 3 -C 8 -cycloalkyl-C 2 -C 8 -alkynyl, C 1- C 8 -alkoxy, C 1 -C 8 -haloalkoxy having 1 to 5 halogen atoms, C 1 -C 8 -alkoxycarbonyl, C 1 -C 8 -haloalkoxy Carbonyl, C 1 -C 8 -alkylsulfenyl, C 2 -C 8 -alkenyloxy, C 3 -C 8 -alkynyloxy, C 3 -C 6 -cycloalkoxy, C 1 -C 8 -alkylsulfinamilide, C 1 -C 8 -alkylsulfonamido, tris (C 1 -C 8 -alkyl) -silyloxy, tris (C 1 -C 8 -alkane ) -Silyl, tri (C 1 -C 8 -alkyl) -silyl-C 2 -C 8 -alkynyl, tri (C 1 -C 8 -alkyl) -silyl-C 2 -C 8 - alkynyloxy, C 6 -C 14 - aryl group, C 6 -C 14 - aryl Alkoxy, C 6 -C 14 - aryl group sulfeno acyl, 5- or 6-membered heteroaryl, or 5- or 6-membered heteroaryl group, wherein the C 6 -C 14 - aryl, C 6- C 14 -aryloxy, C 6 -C 14 -arylsulfenyl, 5- or 6-membered heteroaryl, and 5- or 6-membered heteroaryloxy are unsubstituted or One or more group substitutions selected from halogen, cyanohydrothio, pentafluoro-λ 6 -hydrothio, C 1 -C 8 -alkyl, C 1 -C 8 -haloalkyl, C 1 -C 8 -cyanoalkyl, C 1 -C 8 -alkyloxy, C 1 -C 8 -haloalkyloxy, tris (C 1 -C 8 -alkyl) silyl, tris (C 1- C 8 -alkyl) silyl-C 1 -C 8 -alkyl, C 3 -C 7 -cycloalkyl, C 3 -C 7 -halocycloalkyl, C 3 -C 7 -cycloolefin , C 3 -C 7 -halocycloalkenyl, C 4 -C 10 -cycloalkylalkyl, C 4 -C 10 -halocycloalkylalkyl, C 6 -C 12 -cycloalkyl ring Alkyl, C 1 -C 8 -alkyl-C 3 -C 7 -cycloalkyl, C 1 -C 8 -alkoxy-C 3 -C 7 -cycloalkyl, tri (C 1 -C 8- Alkyl) silyl-C 3 -C 7 -cycloalkyl, C 2 -C 8 -alkenyl, C 2 -C 8 -alkynyl, C 2 -C 8 -alkenyloxy, C 2 -C 8 -Haloalkenyloxy, C 3 -C 8 -alkynyloxy, C 3 -C 8 -halo Alkynyloxy, C 1 -C 8 -cyanoalkoxy, C 4 -C 8 -cycloalkylalkoxy, C 3 -C 6 -cycloalkoxy, C 1 -C 8 -alkyl hydrogen thio, C 1 -C 8 - haloalkyl group hydrogen, C 1 -C 8 - alkylsulfinyl acyl, C 1 -C 8 - acyl halide alkylsulfinyl, C 1 -C 8 - alkoxy Sulfofluorenyl, C 1 -C 8 -haloalkylsulfonyl, C 1 -C 8 -alkylsulfonyloxy, C 1 -C 8 -haloalkylsulfonyloxy, C 1- C 8 -alkoxyalkyl, C 1 -C 8 -alkylthioalkyl, C 1 -C 8 -alkoxyalkoxyalkyl, C 1 -C 8 -haloalkoxyalkyl, Benzyl, phenyl, 5-membered heteroaryl, 6-membered heteroaryl, 6-membered heteroaryloxy, benzyloxy, phenoxy, benzylhydrothio and phenylhydrosulfide base.

X1、X2、X3、X4和X5相互獨立地更佳地係代表氫、鹵素、氰基、C1-C8-烷基、C1-C8-鹵烷基具有1至5個鹵素原子之、C2-C8-烯基、C2-C8-炔基、C3-C8-環烷基-C2-C8-烯基、C3-C8-環烷基-C2-C8-炔基、C1-C8-烷氧基、 C1-C8-鹵基烷氧基具有1至5個鹵素原子之、C6-C14-芳基，或C6-C14-芳基氧基，其中C6-C14-芳基和C6-C14-芳基氧基為未經取代或經一或多個選自下列之基團取代：鹵素、C1-C8-烷基、C1-C8-鹵烷基、C1-C8-烷基氧基和C1-C8-鹵烷基氧基。 X 1 , X 2 , X 3 , X 4 and X 5 independently of one another more preferably represent hydrogen, halogen, cyano, C 1 -C 8 -alkyl, C 1 -C 8 -haloalkyl having 1 to Of 5 halogen atoms, C 2 -C 8 -alkenyl, C 2 -C 8 -alkynyl, C 3 -C 8 -cycloalkyl-C 2 -C 8 -alkenyl, C 3 -C 8 -ring Alkyl-C 2 -C 8 -alkynyl, C 1 -C 8 -alkoxy, C 1 -C 8 -haloalkoxy, C 6 -C 14 -aryl having 1 to 5 halogen atoms , Or C 6 -C 14 -aryloxy, wherein C 6 -C 14 -aryl and C 6 -C 14 -aryloxy are unsubstituted or substituted with one or more groups selected from : Halogen, C 1 -C 8 -alkyl, C 1 -C 8 -haloalkyl, C 1 -C 8 -alkyloxy, and C 1 -C 8 -haloalkyloxy.

X1、X2、X3、X4和X5相互獨立地更佳地係代表氫、氟、氯、溴、氰基、C1-C4-烷基、C1-C4-鹵烷基具有1至5個鹵素原子之、C2-C4-烯基、C2-C4-炔基、C3-C6-環烷基-C2-C4-烯基、C3-C6-環烷基-C2-C4-炔基、C1-C4-烷氧基、C1-C4-鹵基烷氧基具有1至5個鹵素原子之、苯基或苯氧基，其中苯基和苯氧基為未經取代或經一或多個選自下列之基團取代：氟、氯、溴、C1-C4-烷基、C1-C4-鹵烷基、C1-C4-烷基氧基和C1-C4-鹵烷基氧基。 X 1 , X 2 , X 3 , X 4 and X 5 are more independently of each other hydrogen, fluorine, chlorine, bromine, cyano, C 1 -C 4 -alkyl, C 1 -C 4 -halane Group having 1 to 5 halogen atoms, C 2 -C 4 -alkenyl, C 2 -C 4 -alkynyl, C 3 -C 6 -cycloalkyl-C 2 -C 4 -alkenyl, C 3- C 6 -cycloalkyl-C 2 -C 4 -alkynyl, C 1 -C 4 -alkoxy, C 1 -C 4 -haloalkoxy, phenyl or benzene having 1 to 5 halogen atoms Oxygen, wherein phenyl and phenoxy are unsubstituted or substituted with one or more groups selected from the group consisting of fluorine, chlorine, bromine, C 1 -C 4 -alkyl, C 1 -C 4 -halogen Alkyl, C 1 -C 4 -alkyloxy and C 1 -C 4 -haloalkyloxy.

X1、X2、X3、X4和X5相互獨立地更佳地係代表氫、氟、氯、溴、氰基、甲基、乙基、正丙基、異丙基、正丁基、異丁基、第三丁基、CF3、乙烯基、環丙基-C2-C4-炔基、甲氧基、乙氧基、正丙氧基、異丙氧基、正丁氧基、異丁氧基、第三丁氧基、OCF3、苯基或苯氧基，其中苯基和苯氧基為未經取代或經一或多個選自下列之基團取代：氟、氯、溴、甲基、乙基、正丙基、異丙基、正丁基、異丁基、第三丁基和CF3。 X 1 , X 2 , X 3 , X 4 and X 5 are more independently of each other hydrogen, fluorine, chlorine, bromine, cyano, methyl, ethyl, n-propyl, isopropyl, n-butyl , Isobutyl, third butyl, CF 3 , vinyl, cyclopropyl-C 2 -C 4 -alkynyl, methoxy, ethoxy, n-propoxy, isopropoxy, n-butoxy , Isobutoxy, third butoxy, OCF 3 , phenyl, or phenoxy, wherein phenyl and phenoxy are unsubstituted or substituted with one or more groups selected from the group consisting of: fluorine, Chlorine, bromine, methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl, tert-butyl and CF 3 .

X1、X2、X3、X4和X5相互獨立地更佳地係代表氫、氟、氯、溴、氰基、甲基、CF3、乙烯基、環丙基-乙炔基、甲氧基、OCF3、苯基或苯氧基，其中苯基和苯氧基為未經取代或經一或多個選自氟和氯之基團取代。 X 1 , X 2 , X 3 , X 4 and X 5 are more independently of each other hydrogen, fluorine, chlorine, bromine, cyano, methyl, CF 3 , vinyl, cyclopropyl-ethynyl, methyl alkoxy, OCF 3, phenyl or phenoxy, which phenyl and phenoxy is unsubstituted or substituted with one or more substituents selected from the group of fluorine and chlorine substituents.

X1、X2、X3、X4和X5相互獨立地更佳地係代表氫、氟、氯或溴。 X 1 , X 2 , X 3 , X 4 and X 5 are more preferably independent of each other and represent hydrogen, fluorine, chlorine or bromine.

X1、X2、X3、X4和X5相互獨立地更佳地係代表氫、氟或氯。 X 1 , X 2 , X 3 , X 4 and X 5 are more preferably independent of each other and represent hydrogen, fluorine or chlorine.

X1 最佳地係代表氫、氟或氯。 X 1 best represents hydrogen, fluorine or chlorine.

X2 最佳地係代表氫、氟或氯。 X 2 best represents hydrogen, fluorine or chlorine.

X3 更佳地係代表氫、氟或氯、最佳地氫或氯。 X 3 more preferably represents hydrogen, fluorine or chlorine, most preferably hydrogen or chlorine.

X4 更佳地係代表氫、氟或氯、最佳地氫或氟。 X 4 more preferably represents hydrogen, fluorine or chlorine, most preferably hydrogen or fluorine.

X5 更佳地係代表氫、氟或氯、最佳地氫。 X 5 more preferably represents hydrogen, fluorine or chlorine, most preferably hydrogen.

上文籠統所給予的或在較佳範圍內所陳述的基團定義和解釋若需要可彼此組合，亦即包括在特定範圍和較佳範圍之間。其適用於最終產物和對應地析出物和中間物二者。此外，可能不適用於個別定義。 The definitions and explanations of the groups given above or stated in a preferred range may be combined with each other if necessary, that is, included between a specific range and a preferred range. It applies to both the final product and the corresponding precipitates and intermediates. Also, it may not apply to individual definitions.

較佳者係其中各基團係具有上文所提之較佳定義的各個基團的例子。 The preferred is an example in which each group is a group having the preferred definitions mentioned above.

特佳的係給予其中各基團係具有上文所提之更佳及/或最佳定義的各個基團的案例。 Particularly preferred are the cases in which each group is a group with the better and / or best definitions mentioned above.

因此，特佳的為例如式(I)之化合物 Therefore, particularly preferred are compounds of formula (I)

Figure TW201945344A_D0008
其中R1 係代表視需要經鹵素-或C1-C4-烷基-取代的C3-C7-環烷基、視需要經鹵素-或C1-C4-烷基-取代的苯基或視需要經鹵素-或C1-C4-烷基-取代的苯甲基；R2 係代表-OH；R3 係代表氰基或CF3；R4 係代表氫或甲基；R5 係代表氫或甲基；及Q 係代表式(Q-I-1)或(Q-I-2)之6-員芳香環
Figure TW201945344A_D0008
 Representative lines in which R 1 optionally halogen - or C 1 -C 4 - alkyl - substituted C 3 -C 7 - cycloalkyl, optionally halogen - substituted phenyl - or C 1 -C 4 - alkyl Or optionally halogen- or C 1 -C 4 -alkyl-substituted benzyl; R 2 represents -OH; R 3 represents cyano or CF 3 ; R 4 represents hydrogen or methyl; R 5 represents hydrogen or methyl; and Q represents a 6-membered aromatic ring of formula (QI-1) or (QI-2)

Figure TW201945344A_D0009
Figure TW201945344A_D0009

其中 X1、X2、X3、X4和X5相互獨立地係代表氫、鹵素、氰基、C1-C8-烷基、具有1至個鹵素原子之C1-C8-鹵烷基、C2-C8-烯基、C2-C8-炔基、C3-C8-環烷基-C2-C8-烯基、C3-C8-環烷基-C2-C8-炔基、C1-C8-烷氧基、C1-C8-具有1至5個鹵素原子之鹵基烷氧基、C6-C14-芳基或C6-C14-芳基氧基，其中C6-C14-芳基和C6-C14-芳基氧基為未經取代或經一或多個選自下列之基團取代：鹵素、C1-C8-烷基、C1-C8-鹵烷基、C1-C8-烷基氧基和C1-C8-鹵烷基氧基；及其鹽類和N-氧化物。 Wherein X 1 , X 2 , X 3 , X 4 and X 5 independently of one another represent hydrogen, halogen, cyano, C 1 -C 8 -alkyl, C 1 -C 8 -halogen having 1 to halogen atoms Alkyl, C 2 -C 8 -alkenyl, C 2 -C 8 -alkynyl, C 3 -C 8 -cycloalkyl-C 2 -C 8 -alkenyl, C 3 -C 8 -cycloalkyl- C 2 -C 8 -alkynyl, C 1 -C 8 -alkoxy, C 1 -C 8 -halo alkoxy having 1 to 5 halogen atoms, C 6 -C 14 -aryl or C 6 -C 14 -aryloxy, wherein C 6 -C 14 -aryl and C 6 -C 14 -aryloxy are unsubstituted or substituted with one or more groups selected from halogen, C 1- C 8 -alkyl, C 1 -C 8 -haloalkyl, C 1 -C 8 -alkyloxy and C 1 -C 8 -haloalkyloxy; and their salts and N-oxides .

更佳的為式(I)之化合物 More preferred are compounds of formula (I)

Figure TW201945344A_D0010
其中R1 係代表視需要經鹵素-取代的環丙基、視需要經鹵素-取代的苯基或視需要經鹵素-取代的苯甲基；R2 係代表-OH；R3 係代表氰基或CF3；R4 係代表氫或甲基；R5 係代表氫或甲基；及Q 係代表式(Q-I-1)之6-員芳香環
Figure TW201945344A_D0010
 Wherein R 1 represents halogen-substituted cyclopropyl if necessary, halogen-substituted phenyl if necessary, or halogen-substituted benzyl if necessary; R 2 represents -OH; R 3 represents cyano Or CF 3 ; R 4 represents hydrogen or methyl; R 5 represents hydrogen or methyl; and Q represents 6-membered aromatic ring of formula (QI-1)

Figure TW201945344A_D0011
Figure TW201945344A_D0011

其中 X1、X2、X3、X4和X5相互獨立地係代表氫、氟或氯；及其鹽類和N-氧化物。 Wherein X 1 , X 2 , X 3 , X 4 and X 5 independently represent hydrogen, fluorine or chlorine; and salts and N-oxides thereof.

特佳的亦為式(Ia)、(Ib)和(Ic)之化合物 Particularly preferred are compounds of formulae (Ia), (Ib) and (Ic)

Figure TW201945344A_D0012
其中R1 係代表視需要經鹵素-取代的環丙基、視需要經鹵素-取代的苯基或視需要經鹵素-取代的苯甲基，較佳地環丙基、1-氟環丙基、1-氯環丙基、1-溴環丙基、苯基、2-氟苯基、3-氟苯基、4-氟苯基、2,3-二氟苯基、2,4-二氟苯基、2,5-二氟苯基、2,6-二氟苯基、2-氟-3-氯苯基、2-氟-4-氯苯基、2-氟-5-氯苯基、2-氟-6-氯苯基、2-氯-3-氟苯基、2-氯-4-氟苯基、2-氯-5-氟苯基或苯甲基，最佳係1-氟環丙基、1-氯環丙基、2,4-二氟苯基或苯甲基；R3 係代表氰基或CF3；及Q 係代表式(Q-I-1)之6-員芳香環
Figure TW201945344A_D0012
 Wherein R 1 represents halogen-substituted cyclopropyl if necessary, halogen-substituted phenyl if necessary, or halogen-substituted benzyl if necessary, preferably cyclopropyl, 1-fluorocyclopropyl , 1-chlorocyclopropyl, 1-bromocyclopropyl, phenyl, 2-fluorophenyl, 3-fluorophenyl, 4-fluorophenyl, 2,3-difluorophenyl, 2,4-di Fluorophenyl, 2,5-difluorophenyl, 2,6-difluorophenyl, 2-fluoro-3-chlorophenyl, 2-fluoro-4-chlorophenyl, 2-fluoro-5-chlorobenzene Base, 2-fluoro-6-chlorophenyl, 2-chloro-3-fluorophenyl, 2-chloro-4-fluorophenyl, 2-chloro-5-fluorophenyl or benzyl, the best is 1 -Fluorocyclopropyl, 1-chlorocyclopropyl, 2,4-difluorophenyl or benzyl; R 3 represents cyano or CF 3 ; and Q represents 6-membered formula (QI-1) Aromatic ring

Figure TW201945344A_D0013
Figure TW201945344A_D0013

其中X1、X2、X3、X4和X5相互獨立地係代表氫、氟或氯；較佳地苯基、2-氟苯基、3-氟苯基、4-氟苯基、2-氯苯基、3-氯苯基、4-氯苯基、2,3-二氟苯基、2,4-二氟苯基、2,5-二氟苯基、2,6-二氟苯基、2-氟-3-氯苯基、2-氟-4-氯苯基、2-氟-5-氯苯基、2-氟-6-氯苯基、2-氯-3-氟苯基、2-氯-4-氟苯基或2-氯-5-氟苯基， 更佳係苯基、2-氟苯基、2-氯苯基、4-氯苯基、2,3-二氟苯基、2,5-二氟苯基或2-氟-3-氯苯基，最佳係苯基、2-氟苯基或4-氯苯基；及其鹽類和N-氧化物。 Wherein X 1 , X 2 , X 3 , X 4 and X 5 independently represent hydrogen, fluorine or chlorine; preferably phenyl, 2-fluorophenyl, 3-fluorophenyl, 4-fluorophenyl, 2-chlorophenyl, 3-chlorophenyl, 4-chlorophenyl, 2,3-difluorophenyl, 2,4-difluorophenyl, 2,5-difluorophenyl, 2,6-di Fluorophenyl, 2-fluoro-3-chlorophenyl, 2-fluoro-4-chlorophenyl, 2-fluoro-5-chlorophenyl, 2-fluoro-6-chlorophenyl, 2-chloro-3- Fluorophenyl, 2-chloro-4-fluorophenyl or 2-chloro-5-fluorophenyl, more preferably phenyl, 2-fluorophenyl, 2-chlorophenyl, 4-chlorophenyl, 2, 3-difluorophenyl, 2,5-difluorophenyl or 2-fluoro-3-chlorophenyl, preferably phenyl, 2-fluorophenyl or 4-chlorophenyl; and their salts and N -Oxide.

更佳的為式(Ia)、(Ib)和(Ic)之化合物 More preferred are compounds of formulae (Ia), (Ib) and (Ic)

Figure TW201945344A_D0014
其中R1 係代表1-氟環丙基、1-氯環丙基、2,4-二氟苯基或苯甲基；R3 係代表氰基或CF3；及Q 係代表苯基、2-氟苯基、2-氯苯基、4-氯苯基、2,3-二氟苯基、2,5-二氟苯基或2-氟-3-氯苯基，較佳係苯基、2-氟苯基或4-氯苯基；及其鹽類和N-氧化物。
Figure TW201945344A_D0014
 Wherein R 1 represents 1-fluorocyclopropyl, 1-chlorocyclopropyl, 2,4-difluorophenyl or benzyl; R 3 represents cyano or CF 3 ; and Q represents phenyl and 2 -Fluorophenyl, 2-chlorophenyl, 4-chlorophenyl, 2,3-difluorophenyl, 2,5-difluorophenyl or 2-fluoro-3-chlorophenyl, preferably phenyl , 2-fluorophenyl or 4-chlorophenyl; and salts and N-oxides thereof.

在上述化學式和下述化學式中所給與的符號定義，係使用集合名詞。除非在別處另有定義，否則其一般係代表下列取代基：鹵素：氟、氯、溴或碘、較佳地氟、氯或溴。鹵素-取代一般係以字首鹵基、鹵素或鹵素基指出。 Definitions of symbols given in the above chemical formulas and the following chemical formulas use collective nouns. Unless otherwise defined elsewhere, it generally represents the following substituents: halogen: fluorine, chlorine, bromine or iodine, preferably fluorine, chlorine or bromine. Halo-substitution is generally indicated by the prefix halo, halo or halo.

烷基：具有1至8個、較佳地1至6個及更佳地1至4個碳原子之飽和、直鏈或支鏈烴基，例如(但不限於)C1-C6-烷基，例如甲基、乙基、丙基(正丙基)、1-甲基乙基(異丙基)、丁基(正丁基)、1-甲基丙基(第二丁基)、2-甲基丙基(異丁基)、1,1-二甲基乙基(第三丁基)、戊基、1-甲基丁基、2-甲基丁基、3-甲基丁基、2,2-二甲基丙基、1-乙基丙基、1,1-二甲基丙基、1,2-二甲基丙 基、己基、1-甲基戊基、2-甲基戊基、3-甲基戊基、4-甲基戊基、1,1-二甲基丁基、1,2-二甲基丁基、1,3-二甲基丁基、2,2-二甲基丁基、2,3-二甲基丁基、3,3-二甲基丁基、1-乙基丁基、2-乙基丁基、1,1,2-三甲基丙基、1,2,2-三甲基丙基、1-乙基-1-甲基丙基和1-乙基-2-甲基丙基。特言之，該基團為C1-C4-烷基基團，例如甲基、乙基、丙基、1-甲基乙基(異丙基)、丁基、1-甲基丙基(第二丁基)、2-甲基丙基(異丁基)或1,1-二甲基乙基(第三丁基)基團。除非他處另有定義，否則此定義亦適用於作為組合取代基之部分的烷基，例如環烷基烷基、羥基烷基，如，例如烷基氫硫基、烷基亞磺醯基、烷基磺醯基、鹵烷基或鹵烷基氫硫基。 Alkyl: A saturated, straight or branched chain hydrocarbon group having 1 to 8, preferably 1 to 6, and more preferably 1 to 4 carbon atoms, such as (but not limited to) C 1 -C 6 -alkyl , Such as methyl, ethyl, propyl (n-propyl), 1-methylethyl (isopropyl), butyl (n-butyl), 1-methylpropyl (second butyl), 2 -Methylpropyl (isobutyl), 1,1-dimethylethyl (third butyl), pentyl, 1-methylbutyl, 2-methylbutyl, 3-methylbutyl , 2,2-dimethylpropyl, 1-ethylpropyl, 1,1-dimethylpropyl, 1,2-dimethylpropyl, hexyl, 1-methylpentyl, 2-methyl Pentyl, 3-methylpentyl, 4-methylpentyl, 1,1-dimethylbutyl, 1,2-dimethylbutyl, 1,3-dimethylbutyl, 2, 2-dimethylbutyl, 2,3-dimethylbutyl, 3,3-dimethylbutyl, 1-ethylbutyl, 2-ethylbutyl, 1,1,2-trimethyl Propyl, 1,2,2-trimethylpropyl, 1-ethyl-1-methylpropyl and 1-ethyl-2-methylpropyl. In particular, the group is a C 1 -C 4 -alkyl group, such as methyl, ethyl, propyl, 1-methylethyl (isopropyl), butyl, 1-methylpropyl (Second butyl), 2-methylpropyl (isobutyl) or 1,1-dimethylethyl (third butyl) groups. Unless defined elsewhere, this definition also applies to alkyl groups that are part of a combination of substituents, such as cycloalkylalkyl, hydroxyalkyl, such as, for example, alkylhydrothio, alkylsulfinyl, Alkylsulfonyl, haloalkyl or haloalkylhydrothio.

烯基：具有2至8個、較佳地2至6個和更佳地2至4個碳原子及在任何位置具有一個雙鍵之不飽和、直鏈或支鏈烴基，例如(但不限於)C2-C6-烯基，如乙烯基、烯丙基、(E)-2-甲基乙烯基、(Z)-2-甲基乙烯基、異丙烯基、均烯丙基、(E)-丁-2-烯基、(Z)-丁-2-烯基、(E)-丁-1-烯基、(Z)-丁-1-烯基、2-甲基丙-2-烯基、1-甲基丙-2-烯基、2-甲基丙-1-烯基、(E)-1-甲基丙-1-烯基、(Z)-1-甲基丙-1-烯基、戊-4-烯基、(E)-戊-3-烯基、(Z)-戊-3-烯基、(E)-戊-2-烯基、(Z)-戊-2-烯基、(E)-戊-1-烯基、(Z)-戊-1-烯基、3-甲基丁-3-烯基、2-甲基丁-3-烯基、1-甲基丁-3-烯基、3-甲基丁-2-烯基、(E)-2-甲基丁-2-烯基、(Z)-2-甲基丁-2-烯基、(E)-1-甲基丁-2-烯基、(Z)-1-甲基丁-2-烯基、(E)-3-甲基丁-1-烯基、(Z)-3-甲基丁-1-烯基、(E)-2-甲基丁-1-烯基、(Z)-2-甲基丁-1-烯基、(E)-1-甲基丁-1-烯基、(Z)-1-甲基丁-1-烯基、1,1-二甲基丙-2-烯基、1-乙基丙-1-烯基、1-丙基乙烯基、1-異丙基乙烯基、(E)-3,3-二甲基丙-1-烯基、(Z)-3,3-二甲基丙-1-烯基、己-5-烯基、(E)-己-4-烯基、(Z)-己-4-烯基、(E)-己-3-烯基、(Z)-己-3-烯基、(E)-己-2-烯基、(Z)-己-2-烯基、(E)-己-1-烯基、(Z)-己-1-烯基、4-甲基戊-4-烯基、3-甲基戊-4-烯基、2-甲基戊-4-烯基、1-甲基戊-4-烯基、4-甲基戊-3-烯基、(E)-3-甲基戊-3-烯基、(Z)-3-甲基戊-3-烯基、(E)-2-甲基戊-3-烯基、(Z)-2-甲基戊-3-烯基、(E)-1-甲基戊-3-烯基、(Z)-1-甲基戊-3-烯基、(E)-4-甲基戊-2-烯基、(Z)-4-甲基戊-2-烯基、(E)-3-甲基戊-2-烯基、(Z)-3-甲基戊-2-烯基、(E)-2-甲基戊-2-烯基、(Z)-2-甲基戊-2-烯基、(E)-1- 甲基戊-2-烯基、(Z)-1-甲基戊-2-烯基、(E)-4-甲基戊-1-烯基、(Z)-4-甲基戊-1-烯基、(E)-3-甲基戊-1-烯基、(Z)-3-甲基戊-1-烯基、(E)-2-甲基戊-1-烯基、(Z)-2-甲基戊-1-烯基、(E)-1-甲基戊-1-烯基、(Z)-1-甲基戊-1-烯基、3-乙基丁-3-烯基、2-乙基丁-3-烯基、1-乙基丁-3-烯基、(E)-3-乙基丁-2-烯基、(Z)-3-乙基丁-2-烯基、(E)-2-乙基丁-2-烯基、(Z)-2-乙基丁-2-烯基、(E)-1-乙基丁-2-烯基、(Z)-1-乙基丁-2-烯基、(E)-3-乙基丁-1-烯基、(Z)-3-乙基丁-1-烯基、2-乙基丁-1-烯基、(E)-1-乙基丁-1-烯基、(Z)-1-乙基丁-1-烯基、2-丙基丙-2-烯基、1-丙基丙-2-烯基、2-異丙基丙-2-烯基、1-異丙基丙-2-烯基、(E)-2-丙基丙-1-烯基、(Z)-2-丙基丙-1-烯基、(E)-1-丙基丙-1-烯基、(Z)-1-丙基丙-1-烯基、(E)-2-異丙基丙-1-烯基、(Z)-2-異丙基丙-1-烯基、(E)-1-異丙基丙-1-烯基、(Z)-1-異丙基丙-1-烯基、1-(1,1-二甲基乙基)乙烯基、丁-1,3-二烯基、戊-1,4-二烯基、己-1,5-二烯基或甲基己二烯基。特言之，該基團為乙烯基或烯丙基。除非他處另有定義，否則此定義亦適用於作為組合取代基之部分的烯基，例如鹵烯基。 Alkenyl: unsaturated, straight-chain or branched hydrocarbon group having 2 to 8, preferably 2 to 6, and more preferably 2 to 4 carbon atoms and having a double bond at any position, such as (but not limited to) ) C 2 -C 6 -alkenyl, such as vinyl, allyl, (E) -2-methylvinyl, (Z) -2-methylvinyl, isopropenyl, homoallyl, ( E) -But-2-enyl, (Z) -but-2-enyl, (E) -but-1-enyl, (Z) -but-1-enyl, 2-methylpropan-2 -Alkenyl, 1-methylprop-2-enyl, 2-methylprop-1-enyl, (E) -1-methylprop-1-enyl, (Z) -1-methylpropene -1-alkenyl, pent-4-enyl, (E) -pent-3-enyl, (Z) -pent-3-enyl, (E) -pent-2-enyl, (Z)- Pent-2-enyl, (E) -pent-1-enyl, (Z) -pent-1-enyl, 3-methylbut-3-enyl, 2-methylbut-3-enyl , 1-methylbut-3-enyl, 3-methylbut-2-enyl, (E) -2-methylbut-2-enyl, (Z) -2-methylbut-2- Alkenyl, (E) -1-methylbut-2-enyl, (Z) -1-methylbut-2-enyl, (E) -3-methylbut-1-enyl, (Z ) -3-methylbut-1-enyl, (E) -2-methylbut-1-enyl, (Z) -2-methylbut-1-enyl, (E) -1-methyl Butyl-1-enyl, (Z) -1-methylbut-1-enyl, 1,1-dimethylpropan-2-yl Alkenyl, 1-ethylprop-1-enyl, 1-propylvinyl, 1-isopropylvinyl, (E) -3,3-dimethylprop-1-enyl, (Z) -3,3-dimethylprop-1-enyl, hex-5-enyl, (E) -hex-4-enyl, (Z) -hex-4-enyl, (E) -hex- 3-alkenyl, (Z) -hex-3-enyl, (E) -hex-2-enyl, (Z) -hex-2-enyl, (E) -hex-1-enyl, ( Z) -hex-1-enyl, 4-methylpent-4-enyl, 3-methylpent-4-enyl, 2-methylpent-4-enyl, 1-methylpent-4 -Alkenyl, 4-methylpent-3-enyl, (E) -3-methylpent-3-enyl, (Z) -3-methylpent-3-enyl, (E) -2 -Methylpent-3-enyl, (Z) -2-methylpent-3-enyl, (E) -1-methylpent-3-enyl, (Z) -1-methylpent- 3-alkenyl, (E) -4-methylpent-2-enyl, (Z) -4-methylpent-2-enyl, (E) -3-methylpent-2-enyl, (Z) -3-methylpent-2-enyl, (E) -2-methylpent-2-enyl, (Z) -2-methylpent-2-enyl, (E) -1 -Methylpent-2-enyl, (Z) -1-methylpent-2-enyl, (E) -4-methylpent-1-enyl, (Z) -4-methylpent- 1-alkenyl, (E) -3-methylpent-1-enyl, (Z) -3-methylpent-1-enyl, (E) -2-methylpent-1-enyl, (Z) -2-methylpent-1-enyl, (E) -1-methylpent-1-enyl, (Z) -1-methyl Pent-1-enyl, 3-ethylbut-3-enyl, 2-ethylbut-3-enyl, 1-ethylbut-3-enyl, (E) -3-ethylbut- 2-alkenyl, (Z) -3-ethylbut-2-enyl, (E) -2-ethylbut-2-enyl, (Z) -2-ethylbut-2-enyl, (E) -1-ethylbut-2-enyl, (Z) -1-ethylbut-2-enyl, (E) -3-ethylbut-1-enyl, (Z) -3 -Ethylbut-1-enyl, 2-ethylbut-1-enyl, (E) -1-ethylbut-1-enyl, (Z) -1-ethylbut-1-enyl , 2-propylprop-2-enyl, 1-propylprop-2-enyl, 2-isopropylprop-2-enyl, 1-isopropylprop-2-enyl, (E) 2-propylprop-1-enyl, (Z) -2-propylprop-1-enyl, (E) -1-propylprop-1-enyl, (Z) -1-propyl Prop-1-enyl, (E) -2-isopropylprop-1-enyl, (Z) -2-isopropylprop-1-enyl, (E) -1-isopropylprop- 1-alkenyl, (Z) -1-isopropylprop-1-enyl, 1- (1,1-dimethylethyl) vinyl, but-1,3-dienyl, pent-1 , 4-dienyl, hexa-1,5-dienyl or methylhexadienyl. In particular, the group is vinyl or allyl. Unless defined elsewhere, this definition also applies to alkenyl groups such as haloalkenyl as part of a combined substituent.

炔基：具有2至8個，較佳地2至6個和更佳地2至4個碳原子及在任何位置具有一個參鍵之直鏈或支鏈烴基基團，例如(但不限於)C2-C6-炔基，如乙炔基、丙-1-炔基、丙-2-炔基、丁-1-炔基、丁-2-炔基、丁-3-炔基、1-甲基丙-2-炔基、戊-1-炔基、戊-2-炔基、戊-3-炔基、戊-4-炔基、2-甲基丁-3-炔基、1-甲基丁-3-炔基、1-甲基丁-2-炔基、3-甲基丁-1-炔基、1-乙基丙-2-炔基、己-1-炔基、己-2-炔基、己-3-炔基、己-4-炔基、己-5-炔基、3-甲基戊-4-炔基、2-甲基戊-4-炔基、1-甲基戊-4-炔基、2-甲基戊-3-炔基、1-甲基戊-3-炔基、4-甲基戊-2-炔基、1-甲基戊-2-炔基、4-甲基戊-1-炔基、3-甲基戊-1-炔基、2-乙基丁-3-炔基、1-乙基丁-3-炔基、1-乙基丁-2-炔基、1-丙基丙-2-炔基、1-異丙基丙-2-炔基、2,2-二甲基丁-3-炔基、1,1-二甲基丁-3-炔基、1,1-二甲基丁-2-炔基或3,3-二甲基丁-1-炔基基團。特言之，該炔基基團為乙炔基、丙-1-炔基或丙-2-炔基。除非他處另有定義，否則此定義亦適用於作為組合取代基之部分的炔基，例如鹵炔基。 Alkynyl: a straight or branched chain hydrocarbon group having 2 to 8, preferably 2 to 6, and more preferably 2 to 4 carbon atoms, and having a reference bond at any position, such as (but not limited to) C 2 -C 6 -alkynyl, such as ethynyl, prop-1-ynyl, prop-2-ynyl, but-1-ynyl, but-2-ynyl, but-3-ynyl, 1- Methylprop-2-ynyl, pent-1-ynyl, pent-2-ynyl, pent-3-ynyl, pent-4-ynyl, 2-methylbut-3-ynyl, 1- Methylbut-3-ynyl, 1-methylbut-2-ynyl, 3-methylbut-1-ynyl, 1-ethylprop-2-ynyl, hex-1-ynyl, hexyl -2-alkynyl, hex-3-alkynyl, hex-4-alkynyl, hex-5-alkynyl, 3-methylpent-4-ynyl, 2-methylpent-4-ynyl, 1 -Methylpent-4-ynyl, 2-methylpent-3-ynyl, 1-methylpent-3-ynyl, 4-methylpent-2-ynyl, 1-methylpent-2 -Alkynyl, 4-methylpent-1-ynyl, 3-methylpent-1-ynyl, 2-ethylbut-3-ynyl, 1-ethylbut-3-ynyl, 1- Ethylbut-2-ynyl, 1-propylprop-2-ynyl, 1-isopropylprop-2-ynyl, 2,2-dimethylbut-3-ynyl, 1,1- A dimethylbut-3-ynyl, 1,1-dimethylbut-2-ynyl or 3,3-dimethylbut-1-ynyl group. In particular, the alkynyl group is ethynyl, prop-1-ynyl or prop-2-ynyl. Unless otherwise defined elsewhere, this definition also applies to alkynyls such as haloalkynyls that are part of a combined substituent.

烷氧基：具有1至8個、較佳地1至6個及更佳地1至4個碳原子之飽和、直鏈或支鏈烷氧基，例如(但不限於)C1-C6-烷氧基，如甲氧基、乙氧基、丙氧基、1-甲基乙氧基、丁氧基、1-甲基丙氧基、2-甲基丙氧基、1,1-二甲基乙氧基、戊氧基、1-甲基丁氧基、2-甲基丁氧基、3-甲基丁氧基、2,2-二甲基丙氧基、1-乙基丙氧基、1,1-二甲基丙氧基、1,2-二甲基丙氧基、己氧基、1-甲基戊氧基、2-甲基戊氧基、3-甲基戊氧基、4-甲基戊氧基、1,1-二甲基丁氧基、1,2-二甲基丁氧基、1,3-二甲基丁氧基、2,2-二甲基丁氧基、2,3-二甲基丁氧基、3,3-二甲基丁氧基、1-乙基丁氧基、2-乙基丁氧基、1,1,2-三甲基丙氧基、1,2,2-三甲基丙氧基、1-乙基-1-甲基丙氧基和1-乙基-2-甲基丙氧基。除非他處另有定義，否則此定義亦適用於作為組合取代基之部分的烷氧基，例如鹵基烷氧基、炔基烷氧基。 Alkoxy: a saturated, straight-chain or branched alkoxy group having 1 to 8, preferably 1 to 6, and more preferably 1 to 4 carbon atoms, such as (but not limited to) C 1 -C 6 -Alkoxy, such as methoxy, ethoxy, propoxy, 1-methylethoxy, butoxy, 1-methylpropoxy, 2-methylpropoxy, 1,1- Dimethylethoxy, pentyloxy, 1-methylbutoxy, 2-methylbutoxy, 3-methylbutoxy, 2,2-dimethylpropoxy, 1-ethyl Propoxy, 1,1-dimethylpropoxy, 1,2-dimethylpropoxy, hexyloxy, 1-methylpentoxy, 2-methylpentoxy, 3-methyl Pentyloxy, 4-methylpentyloxy, 1,1-dimethylbutoxy, 1,2-dimethylbutoxy, 1,3-dimethylbutoxy, 2,2-di Methylbutoxy, 2,3-dimethylbutoxy, 3,3-dimethylbutoxy, 1-ethylbutoxy, 2-ethylbutoxy, 1,1,2- Trimethylpropoxy, 1,2,2-trimethylpropoxy, 1-ethyl-1-methylpropoxy and 1-ethyl-2-methylpropoxy. Unless otherwise defined elsewhere, this definition also applies to alkoxy groups that are part of a combined substituent, such as haloalkoxy, alkynylalkoxy.

烷氧基羰基：具有1至8個，較佳地1至6個及更佳地1至4個碳原子(如上所述)且經由羰基基團(-C(=O)-)與主架構鍵結之烷氧基。除非他處另有定義，否則此定義亦適用於作為組合取代基之部分的烷氧基羰基，例如環烷基烷氧基羰基。 Alkoxycarbonyl: has 1 to 8, preferably 1 to 6 and more preferably 1 to 4 carbon atoms (as described above) and via the carbonyl group (-C (= O)-) and the main structure Bonded alkoxy. Unless otherwise defined elsewhere, this definition also applies to alkoxycarbonyl groups that are part of a combined substituent, such as cycloalkylalkoxycarbonyl.

烷基氫硫基：具有1至8個、較佳地1至6個及更佳地1至4個碳原子之飽和、直鏈或支鏈烷基氫硫基，例如(但不限於)C1-C6-烷基氫硫基，如甲基氫硫基、乙基氫硫基、丙基氫硫基、1-甲基乙基氫硫基、丁基氫硫基、1-甲基丙基氫硫基、2-甲基丙基氫硫基、1,1-二甲基乙基氫硫基、戊基氫硫基、1-甲基丁基氫硫基、2-甲基丁基氫硫基、3-甲基丁基氫硫基、2,2-二甲基丙基氫硫基、1-乙基丙基氫硫基、1,1-二甲基丙基氫硫基、1,2-二甲基丙基氫硫基、己基氫硫基、1-甲基戊基氫硫基、2-甲基戊基氫硫基、3-甲基戊基氫硫基、4-甲基戊基氫硫基、1,1-二甲基丁基氫硫基、1,2-二甲基丁基氫硫基、1,3-二甲基丁基氫硫基、2,2-二甲基丁基氫硫基、2,3-二甲基丁基氫硫基、3,3-二甲基丁基氫硫基、1-乙基丁基氫硫基、2-乙基丁基氫硫基、1,1,2-三甲基丙基氫硫基、1,2,2-三甲基丙基氫硫基、1-乙基-1-甲基丙基氫硫基和1-乙基-2-甲基丙基氫硫基。除非他處另有定義，否則此定義亦適用於作為組合取代基之部分的烷基氫硫基，例如鹵烷基氫硫基。 Alkylhydrosulfanyl: A saturated, straight-chain or branched alkylhydrosulfanyl group having 1 to 8, preferably 1 to 6, and more preferably 1 to 4 carbon atoms, such as (but not limited to) C 1 -C 6 -alkylhydrothio, such as methylhydrothio, ethylhydrothio, propylhydrothio, 1-methylethylhydrothio, butylhydrothio, 1-methyl Propylhydrothio, 2-methylpropylhydrothio, 1,1-dimethylethylhydrothio, pentylhydrothio, 1-methylbutylhydrothio, 2-methylbutyl Hydroxythio, 3-methylbutylhydrothio, 2,2-dimethylpropylhydrothio, 1-ethylpropylhydrothio, 1,1-dimethylpropylhydrothio , 1,2-dimethylpropylhydrosulfanyl, hexylhydrosulfanyl, 1-methylpentylhydrosulfanyl, 2-methylpentylhydrosulfanyl, 3-methylpentylhydrosulfanyl, 4 -Methylpentylhydrosulfanyl, 1,1-dimethylbutylhydrosulfanyl, 1,2-dimethylbutylhydrosulfanyl, 1,3-dimethylbutylhydrosulfanyl, 2, 2-dimethylbutylhydrosulfanyl, 2,3-dimethylbutylhydrosulfanyl, 3,3-dimethylbutylhydrosulfanyl, 1-ethylbutylhydrosulfanyl, 2-ethyl Butyl sulfhydryl, 1,1,2-trimethylpropyl sulfhydryl, 1,2,2-trimethylpropyl sulfhydryl, 1 -Ethyl-1-methylpropylhydrothio and 1-ethyl-2-methylpropylhydrothio. Unless defined elsewhere, this definition also applies to alkylhydrosulfanyl groups, such as haloalkylhydrosulfanyl groups, which are part of a combined substituent.

烷基亞磺醯基：具有1至8個、較佳地1至6個及更佳地1至4個碳原子之飽和、直鏈或支鏈烷基亞磺醯基，例如(但不限於)C1-C6-烷基亞磺醯基，如甲基亞磺醯基、乙基亞磺醯基、丙基亞磺醯基、1-甲基乙基亞磺醯基、丁基亞磺醯基、1-甲基丙基亞磺醯基、2-甲基丙基亞磺醯基、1,1-二甲基乙基亞磺醯基、戊基亞磺醯基、1-甲基丁基亞磺醯基、2-甲基丁基亞磺醯基、3-甲基丁基亞磺醯基、2,2-二甲基丙基亞磺醯基、1-乙基丙基亞磺醯基、1,1-二甲基丙基亞磺醯基、1,2-二甲基丙基亞磺醯基、己基亞磺醯基、1-甲基戊基亞磺醯基、2-甲基戊基亞磺醯基、3-甲基戊基亞磺醯基、4-甲基戊基亞磺醯基、1,1-二甲基丁基亞磺醯基、1,2-二甲基丁基亞磺醯基、1,3-二甲基丁基亞磺醯基、2,2-二甲基丁基亞磺醯基、2,3-二甲基丁基亞磺醯基、3,3-二甲基丁基亞磺醯基、1-乙基丁基亞磺醯基、2-乙基丁基亞磺醯基、1,1,2-三甲基丙基亞磺醯基、1,2,2-三甲基丙基亞磺醯基、1-乙基-1-甲基丙基亞磺醯基和1-乙基-2-甲基丙基亞磺醯基。除非他處另有定義，否則此定義亦適用於作為組合取代基之部分的烷基亞磺醯基，例如鹵烷基亞磺醯基。 Alkylsulfinylsulfenyl: A saturated, straight-chain or branched alkylsulfinylene having 1 to 8, preferably 1 to 6, and more preferably 1 to 4 carbon atoms, such as (but not limited to) ) C 1 -C 6 -alkylsulfinyl sulfenyl, such as methylsulfinyl, ethylsulfinyl, propylsulfinyl, 1-methylethylsulfinyl, butylsulfinyl Sulfonyl, 1-methylpropylsulfinyl, 2-methylpropylsulfinyl, 1,1-dimethylethylsulfinyl, pentylsulfinyl, 1-methyl Butylsulfinyl sulfenyl, 2-methylbutylsulfinyl sulfinyl, 3-methylbutylsulfinyl sulfinyl, 2,2-dimethylpropylsulfinyl sulfinyl, 1-ethylpropyl Sulfinyl sulfenyl, 1,1-dimethylpropylsulfinyl sulfinyl, 1,2-dimethylpropylsulfinyl sulfinyl, hexylsulfinyl sulfinyl, 1-methylpentylsulfinyl sulfinyl, 2-methylpentylsulfinyl sulfenyl, 3-methylpentylsulfinyl sulfinyl, 4-methylpentylsulfinyl sulfinyl, 1,1-dimethylbutylsulfinyl sulfinyl, 1,2 -Dimethylbutylsulfinyl sulfenyl, 1,3-dimethylbutylsulfinyl sulfinyl, 2,2-dimethylbutylsulfinyl sulfinyl, 2,3-dimethylbutylsulfinyl Fluorenyl, 3,3-dimethylbutylsulfinylene, 1-ethylbutylsulfinylene, 2-ethylbutylsulfinyl sulfenyl, 1,1,2-trimethylpropylsulfinyl sulfinyl, 1,2,2-trimethylpropylsulfinyl sulfinyl, 1-ethyl-1- Methylpropylsulfinyl and 1-ethyl-2-methylpropylsulfinyl. Unless otherwise defined elsewhere, this definition also applies to alkylsulfinyl sulfenyl as part of a combination of substituents, such as haloalkylsulfinyl sulfinyl.

烷基磺醯基：具有1至8個、較佳地1至6個及更佳地1至4個碳原子之飽和、直鏈或支鏈烷基磺醯基，例如(但不限於)C1-C6-烷基磺醯基，如甲基磺醯基、乙基磺醯基、丙基磺醯基、1-甲基乙基磺醯基、丁基磺醯基、1-甲基丙基-磺醯基、2-甲基丙基磺醯基、1,1-二甲基乙基磺醯基、戊基磺醯基、1-甲基丁基磺醯基、2-甲基丁基磺醯基、3-甲基丁基磺醯基、2,2-二甲基丙基磺醯基、1-乙基丙基磺醯基、1,1-二甲基丙基磺醯基、1,2-二甲基丙基磺醯基、己基磺醯基、1-甲基戊基磺醯基、2-甲基戊基磺醯基、3-甲基戊基磺醯基、4-甲基戊基磺醯基、1,1-二甲基丁基磺醯基、1,2-二甲基丁基磺醯基、1,3-二甲基丁基磺醯基、2,2-二甲基丁基磺醯基、2,3-二甲基丁基磺醯基、3,3-二甲基丁基磺醯基、1-乙基丁基磺醯基、2-乙基丁基磺醯基、1,1,2-三甲基丙基磺醯基、1,2,2-三甲基丙基磺醯基、1-乙基-1-甲基丙基磺醯基和1-乙基-2-甲基丙基磺醯基。除非他處另有定義，否則此定義亦適用於作為組合取代基之部分的烷基磺醯基，例如烷基磺醯基烷基。 Alkylsulfonyl: Saturated, straight-chain or branched alkylsulfonyl having 1 to 8, preferably 1 to 6, and more preferably 1 to 4 carbon atoms, such as (but not limited to) C 1 -C 6 -alkylsulfonyl, such as methylsulfonyl, ethylsulfonyl, propylsulfonyl, 1-methylethylsulfonyl, butylsulfonyl, 1-methyl Propyl-sulfonyl, 2-methylpropylsulfonyl, 1,1-dimethylethylsulfonyl, pentylsulfonyl, 1-methylbutylsulfonyl, 2-methyl Butylsulfonyl, 3-methylbutylsulfonyl, 2,2-dimethylpropylsulfonyl, 1-ethylpropylsulfonyl, 1,1-dimethylpropylsulfonyl , 1,2-dimethylpropylsulfonyl, hexylsulfonyl, 1-methylpentylsulfonyl, 2-methylpentylsulfonyl, 3-methylpentylsulfonyl, 4-methylpentylsulfonyl, 1,1-dimethylbutylsulfonyl, 1,2-dimethylbutylsulfonyl, 1,3-dimethylbutylsulfonyl, 2 2,2-dimethylbutylsulfonyl, 2,3-dimethylbutylsulfonyl, 3,3-dimethylbutylsulfonyl, 1-ethylbutylsulfonyl, 2- Ethylbutylsulfonyl, 1,1,2-trimethylpropylsulfonyl, 1,2,2-trimethylpropylsulfonyl, 1-ethyl-1-methylpropylsulfonyl and 1-ethyl-2-methylpropylsulfonyl. Unless otherwise defined elsewhere, this definition also applies to alkylsulfonyl groups, such as alkylsulfonylalkyl, as part of a combination of substituents.

單烷基胺基係代表具有一個帶有1至4個碳原子的烷基殘基與氮原子相連接之胺基。非限定實例包括甲基胺基、乙基胺基、正丙基胺基、異丙基胺基、正丁基胺基和第三丁基胺基。 The monoalkylamino group represents an amine group having an alkyl residue having 1 to 4 carbon atoms connected to a nitrogen atom. Non-limiting examples include methylamino, ethylamino, n-propylamino, isopropylamino, n-butylamino, and tert-butylamino.

二烷基胺基係代表具有二個獨立選自含1至4個碳原子的烷基殘基與氮原子相連接之胺基。非限定實例包括N,N-二甲基胺基、N,N-二乙基胺基、N,N-二異丙基胺基、N-乙基-N-甲基胺基、N-甲基-N-正丙基胺基、N-異丙基-N-正丙基胺基和N-第三丁基-N-甲基胺基。 The dialkylamino group represents an amine group having two independently selected from an alkyl residue having 1 to 4 carbon atoms and having a nitrogen atom attached thereto. Non-limiting examples include N, N -dimethylamino, N, N -diethylamino, N, N -diisopropylamino, N -ethyl- N -methylamino, N -methyl -N -n-propylamino, N -isopropyl- N -n-propylamino and N -tert-butyl- N -methylamino.

環烷基：具有3至10個、較佳地3至8個及更佳地3至6個碳環成員之單環、飽和烴基基團，例如(但不限於)環丙基、環戊基和環己基。除非他處另有定義，否則此定義亦適用於作為組合取代基之部分的環烷基，例如環烷基烷基。 Cycloalkyl: a monocyclic, saturated hydrocarbon group having 3 to 10, preferably 3 to 8 and more preferably 3 to 6 carbocyclic members, such as (but not limited to) cyclopropyl, cyclopentyl And cyclohexyl. Unless otherwise defined elsewhere, this definition also applies to cycloalkyls such as cycloalkylalkyls that are part of a combined substituent.

環烯基：具有3至10個，較佳地3至8個及更佳地3至6個碳環成員之單環、部分不飽和烴基基團，例如(但不限於)環丙烯、環戊烯和環己烯。 除非他處另有定義，否則此定義亦適用於作為組合取代基之部分的環烯基，例如環烯基烷基。 Cycloalkenyl: a monocyclic, partially unsaturated hydrocarbon group having 3 to 10, preferably 3 to 8 and more preferably 3 to 6 carbocyclic members, such as (but not limited to) cyclopropene, cyclopentyl Ene and cyclohexene. Unless otherwise defined elsewhere, this definition also applies to cycloalkenyl, such as cycloalkenylalkyl, as part of a combined substituent.

環烷氧基：具有3至10個，較佳地3至8個及更佳地3至6個碳環成員之單環、飽和環烷基氧基，例如(但不限於)環丙氧基、環戊氧基和環己氧基。除非他處另有定義，否則此定義亦適用於作為組合取代基之部分的環烷氧基，例如環烷氧基烷基。 Cycloalkoxy: a monocyclic, saturated cycloalkyloxy group having 3 to 10, preferably 3 to 8 and more preferably 3 to 6 carbocyclic members, such as (but not limited to) cyclopropoxy , Cyclopentyloxy and cyclohexyloxy. Unless defined elsewhere, this definition also applies to cycloalkoxy groups, such as cycloalkoxyalkyl, as part of a combination of substituents.

鹵烷基：具有1至8個、較佳地1至6個及更佳地1至4個碳原子(如上述)之直鏈或支鏈烷基基團，其中這些基團的某些或所有的氫被如上所述之鹵素原子取代，例如(但不限於)C1-C3-鹵烷基，如氯甲基、溴甲基、二氯甲基、三氯甲基、氟甲基、二氟甲基、三氟甲基、氯氟甲基、二氯氟甲基、氯二氟甲基、1-氯乙基、1-溴乙基、1-氟乙基、2-氟乙基、2,2-二氟乙基、2,2,2-三氟乙基、2-氯-2-氟乙基、2-氯-2,2-二氟乙基、2,2-二氯-2-氟乙基、2,2,2-三氯乙基、五氟乙基和1,1,1-三氟丙-2-基。除非他處另有定義，否則此定義亦適用於作為組合取代基之部分的鹵烷基，例如鹵烷基胺基烷基。 Haloalkyl: a straight or branched chain alkyl group having 1 to 8, preferably 1 to 6, and more preferably 1 to 4 carbon atoms (as described above), wherein some of these groups or All hydrogens are replaced by halogen atoms as described above, such as (but not limited to) C 1 -C 3 -haloalkyl, such as chloromethyl, bromomethyl, dichloromethyl, trichloromethyl, fluoromethyl , Difluoromethyl, trifluoromethyl, chlorofluoromethyl, dichlorofluoromethyl, chlorodifluoromethyl, 1-chloroethyl, 1-bromoethyl, 1-fluoroethyl, 2-fluoroethyl Radical, 2,2-difluoroethyl, 2,2,2-trifluoroethyl, 2-chloro-2-fluoroethyl, 2-chloro-2,2-difluoroethyl, 2,2-di Chloro-2-fluoroethyl, 2,2,2-trichloroethyl, pentafluoroethyl and 1,1,1-trifluoroprop-2-yl. Unless otherwise defined elsewhere, this definition also applies to haloalkyls, such as haloalkylaminoalkyl, as part of a combination of substituents.

鹵基烯基和鹵基炔基定義係類似鹵烷基，但是係以烯基和炔基存在作為取代基的一部分，取代烷基基團。 The definition of haloalkenyl and haloalkynyl is similar to haloalkyl, but it replaces alkyl group with alkenyl and alkynyl as part of the substituent.

鹵基烷氧基：具有1至8個、較佳地1至6個及更佳地1至4個碳原子之直鏈或支鏈烷氧基(如上述)，其中這些基團的某些或所有的氫被如上所述之鹵素原子取代，例如(但不限於)C1-C3-鹵基烷氧基，如氯甲氧基、溴甲氧基、二氯甲氧基、三氯甲氧基、氟甲氧基、二氟甲氧基、三氟甲氧基、氯氟甲氧基、二氯氟甲氧基、氯二氟甲氧基、1-氯乙氧基、1-溴乙氧基、1-氟乙氧基、2-氟乙氧基、2,2-二氟乙氧基、2,2,2-三氟乙氧基、2-氯-2-氟乙氧基、2-氯-2,2-二氟乙氧基、2,2-二氯-2-氟乙氧基、2,2,2-三氯乙氧基、五氟乙氧基和1,1,1-三氟丙-2-氧基。除非他處另有定義，否則此定義亦適用於作為組合取代基之部分的鹵基烷氧基，例如鹵基烷氧基烷基。 Haloalkoxy: a straight or branched chain alkoxy group having 1 to 8, preferably 1 to 6, and more preferably 1 to 4 carbon atoms (as described above), of which some of these groups Or all hydrogens are replaced by halogen atoms as described above, such as (but not limited to) C 1 -C 3 -haloalkoxy, such as chloromethoxy, bromomethoxy, dichloromethoxy, trichloro Methoxy, fluoromethoxy, difluoromethoxy, trifluoromethoxy, chlorofluoromethoxy, dichlorofluoromethoxy, chlorodifluoromethoxy, 1-chloroethoxy, 1- Bromoethoxy, 1-fluoroethoxy, 2-fluoroethoxy, 2,2-difluoroethoxy, 2,2,2-trifluoroethoxy, 2-chloro-2-fluoroethoxy Base, 2-chloro-2,2-difluoroethoxy, 2,2-dichloro-2-fluoroethoxy, 2,2,2-trichloroethoxy, pentafluoroethoxy and 1, 1,1-trifluoroprop-2-oxy. Unless otherwise defined elsewhere, this definition also applies to haloalkoxy groups such as haloalkoxyalkyl as part of a combined substituent.

鹵烷基氫硫基：具有1至8個，較佳地1至6個及更佳地1至4個碳原子之直鏈或支鏈烷基氫硫基基團(如上述)，其中這些基團的某些或所有的氫被如上所述之鹵素原子取代，例如(但不限於)C1-C3-鹵烷基氫硫基，如氯甲基氫硫基、溴甲基氫硫基、二氯甲基氫硫基、三氯甲基氫硫基、氟甲基氫硫基、二氟甲基氫硫基、三氟甲基氫硫基、氯氟甲基氫硫基、二氯氟甲基氫硫基、氯二氟甲基氫硫基、1-氯乙基氫硫基、1-溴乙基氫硫基、1-氟乙基氫硫基、2-氟乙基氫硫基、2,2-二氟乙基氫硫基、2,2,2-三氟乙基氫硫基、2-氯-2-氟乙基氫硫基、2-氯-2,2-二氟乙基氫硫基、2,2-二氯-2-氟乙基氫硫基、2,2,2-三氯乙基氫硫基、五氟乙基氫硫基和1,1,1-三氟丙-2-基氫硫基。除非他處另有定義，否則此定義亦適用於作為組合取代基之部分的鹵烷基氫硫基，例如鹵烷基氫硫基烷基。 Haloalkylhydrosulfanyl: a straight or branched chain alkylhydrosulfanyl group having 1 to 8, preferably 1 to 6, and more preferably 1 to 4 carbon atoms (as described above), wherein these Some or all of the hydrogens of the group are replaced by a halogen atom as described above, such as (but not limited to) C 1 -C 3 -haloalkylhydrothio, such as chloromethylhydrothio, bromomethylhydrosulfide Base, dichloromethylhydrosulfanyl, trichloromethylhydrosulfanyl, fluoromethylhydrosulfanyl, difluoromethylhydrosulfanyl, trifluoromethylhydrosulfanyl, chlorofluoromethylhydrosulfanyl, Chlorofluoromethylhydrosulfanyl, chlorodifluoromethylhydrosulfanyl, 1-chloroethylhydrosulfanyl, 1-bromoethylhydrosulfanyl, 1-fluoroethylhydrosulfanyl, 2-fluoroethylhydrogen Thio, 2,2-difluoroethylhydrothio, 2,2,2-trifluoroethylhydrothio, 2-chloro-2-fluoroethylhydrothio, 2-chloro-2,2- Difluoroethylhydrosulfanyl, 2,2-dichloro-2-fluoroethylhydrosulfanyl, 2,2,2-trichloroethylhydrosulfanyl, pentafluoroethylhydrosulfanyl, and 1,1, 1-trifluoroprop-2-ylhydrothio. Unless otherwise defined elsewhere, this definition also applies to haloalkylhydrothio, as part of a combination of substituents, such as haloalkylhydrothioalkyl.

芳基：具有6至14個碳原子之單-、雙-或三環芳香或部分芳香基團，例如(但不限於)苯基、萘基、四氫萘基、茚基和二氫茚基。與上級通式結構之鍵結可經由芳基殘基之任何可能的環成員來進行。芳基較佳地係選自苯基、1-萘基和2-萘基。苯基為特佳的。 Aryl: A mono-, bi-, or tricyclic aromatic or partially aromatic group having 6 to 14 carbon atoms, such as (but not limited to) phenyl, naphthyl, tetrahydronaphthyl, indenyl, and dihydroindenyl . Bonding to the general structure can be carried out via any possible ring member of the aryl residue. Aryl is preferably selected from phenyl, 1-naphthyl and 2-naphthyl. Phenyl is particularly preferred.

雜芳基：含有至少1個，若適當的話，含有2、3、4或5個雜原子之5或6-員環狀芳香基團，其中該雜原子彼此相互獨立地係選自S、N和O之 群，且該基團亦可為具有至多14個環成員之雙-或三環系的一部分，其中可與一或二個另外的環烷基、環烯基、雜環基、芳基及/或雜芳基殘基形成該環系統，且其中苯并稠合5或6-員雜芳基基團為較佳的。與上級通式結構之鍵結可經由雜芳基殘基之任何可能的環成員來進行。經由碳環成員之一者與主幹相連接的5-員雜芳基基團之實例有呋喃-2-基、呋喃-3-基、噻吩-2-基、噻吩-3-基、吡咯-2-基、吡咯-3-基、異

Figure TW201945344A_D0015
唑-3-基、異
Figure TW201945344A_D0016
唑-4-基、異
Figure TW201945344A_D0017
唑-5-基、異噻唑-3-基、異噻唑-4-基、異噻唑-5-基、吡唑-3-基、吡唑-4-基、吡唑-5-基、
Figure TW201945344A_D0018
唑-2-基、
Figure TW201945344A_D0019
唑-4-基、
Figure TW201945344A_D0020
唑-5-基、噻唑-2-基、噻唑-4-基、噻唑-5-基、咪唑-2-基、咪唑-4-基、1,2,4-
Figure TW201945344A_D0021
二唑-3-基、1,2,4-
Figure TW201945344A_D0022
二唑-5-基、1,2,4-噻二唑-3-基、1,2,4-噻二唑-5-基、1,2,4-三唑-3-基、1,3,4-
Figure TW201945344A_D0023
二唑-2-基、1,3,4-噻二唑-2-基和1,3,4-三唑-2-基。經由氮環成員與主幹相連結的5-員雜芳基基團有吡咯-1-基、吡唑-1-基、1,2,4-三唑-1-基、咪唑-1-基、1,2,3-三唑-1-基和1,3,4-三唑-1-基。6-員雜芳基基團之實例有吡啶-2-基、吡啶-3-基、吡啶-4-基、嗒
Figure TW201945344A_D0024
-3-基、嗒
Figure TW201945344A_D0025
-4-基、嘧啶-2-基、嘧啶-4-基、嘧啶-5-基、吡
Figure TW201945344A_D0026
-2-基、1,3,5-三
Figure TW201945344A_D0027
-2-基、1,2,4-三
Figure TW201945344A_D0028
-3-基和1,2,4,5-四
Figure TW201945344A_D0029
-3-基。苯并稠合5-員雜芳基基團之實例有吲哚-1-基、吲哚-2-基、吲哚-3-基、吲哚-4-基、吲哚-5-基、吲哚-6-基、吲哚-7-基、苯并咪唑-1-基、苯并咪唑-2-基、苯并咪唑-4-基、苯并咪唑-5-基、吲唑-1-基、吲唑-3-基、吲唑-4-基、吲唑-5-基、吲唑-6-基、吲唑-7-基、吲唑-2-基、1-苯并呋喃-2-基、1-苯并呋喃-3-基、1-苯并呋喃-4-基、1-苯并呋喃-5-基、1-苯并呋喃-6-基、1-苯并呋喃-7-基、1-苯并噻吩-2-基、1-苯并噻吩-3-基、1-苯并噻吩-4-基、1-苯并噻吩-5-基、1-苯并噻吩-6-基、1-苯并噻吩-7-基、1,3-苯并噻唑-2-基、1,3-苯并噻唑-4-基、1,3-苯并噻唑-5-基、1,3-苯并噻唑-6-基、1,3-苯并噻唑-7-基、1,3-苯并
Figure TW201945344A_D0030
唑-2-基、1,3-苯并
Figure TW201945344A_D0031
唑-4-基、1,3-苯并
Figure TW201945344A_D0032
唑-5-基、1,3-苯并
Figure TW201945344A_D0033
唑-6-基和1,3-苯并
Figure TW201945344A_D0034
唑-7-基。苯并稠合6-員雜芳基基團之實例有喹啉-2-基、喹啉-3-基、喹啉-4-基、喹啉-5-基、喹啉-6-基、喹啉-7-基、喹啉-8-基、異喹啉-1-基、異喹啉-3-基、異喹啉-4-基、異喹啉-5-基、異喹啉-6-基、異喹啉-7-基和異喹啉-8-基。作為雙環系部分之5-或6-員雜芳基的另外實例有1,2,3,4-四氫喹啉-1-基、1,2,3,4-四氫喹啉 -2-基、1,2,3,4-四氫喹啉-7-基、1,2,3,4-四氫喹啉-8-基、1,2,3,4-四氫異喹啉-1-基、1,2,3,4-四氫異喹啉-2-基、1,2,3,4-四氫異喹啉-5-基、1,2,3,4-四氫異喹啉-6-基和1,2,3,4-四氫異喹啉-7-基。除非他處另有定義，否則此定義亦適用於作為組合取代基之部分的雜芳基，例如雜芳烷基。 Heteroaryl: a 5 or 6-membered cyclic aromatic group containing at least one, if appropriate, two, three, four, or five heteroatoms, wherein the heteroatoms are independently selected from S, N And O, and the group may also be part of a bi- or tricyclic system having up to 14 ring members, which may be associated with one or two additional cycloalkyl, cycloalkenyl, heterocyclyl, aromatic And / or heteroaryl residues form the ring system, with benzo-fused 5 or 6-membered heteroaryl groups being preferred. Bonding to the general structure can be carried out via any possible ring member of the heteroaryl residue. Examples of 5-membered heteroaryl groups connected to the backbone via one of the carbocyclic members are furan-2-yl, furan-3-yl, thien-2-yl, thien-3-yl, pyrrole-2 -Yl, pyrrol-3-yl, iso
Figure TW201945344A_D0015
Azol-3-yl, iso
Figure TW201945344A_D0016
Azole-4-yl, iso
Figure TW201945344A_D0017
Azol-5-yl, isothiazol-3-yl, isothiazol-4-yl, isothiazol-5-yl, pyrazol-3-yl, pyrazol-4-yl, pyrazol-5-yl,
Figure TW201945344A_D0018
Azole-2-yl,
Figure TW201945344A_D0019
Azole-4-yl,
Figure TW201945344A_D0020
Azole-5-yl, thiazol-2-yl, thiazol-4-yl, thiazol-5-yl, imidazol-2-yl, imidazol-4-yl, 1, 2, 4-
Figure TW201945344A_D0021
Diazol-3-yl, 1,2,4-
Figure TW201945344A_D0022
Diazol-5-yl, 1,2,4-thiadiazol-3-yl, 1,2,4-thiadiazol-5-yl, 1,2,4-triazol-3-yl, 1, 3,4-
Figure TW201945344A_D0023
Diazol-2-yl, 1,3,4-thiadiazol-2-yl and 1,3,4-triazol-2-yl. 5-membered heteroaryl groups connected to the backbone via nitrogen ring members are pyrrol-1-yl, pyrazol-1-yl, 1,2,4-triazol-1-yl, imidazol-1-yl, 1,2,3-triazol-1-yl and 1,3,4-triazol-1-yl. Examples of 6-membered heteroaryl groups are pyridin-2-yl, pyridin-3-yl, pyridin-4-yl,
Figure TW201945344A_D0024
-3-yl, da
Figure TW201945344A_D0025
4-yl, pyrimidin-2-yl, pyrimidin-4-yl, pyrimidin-5-yl, pyridine
Figure TW201945344A_D0026
-2-yl, 1,3,5-tri
Figure TW201945344A_D0027
-2-yl, 1,2,4-tri
Figure TW201945344A_D0028
-3-yl and 1,2,4,5-tetra
Figure TW201945344A_D0029
-3-yl. Examples of benzo-fused 5-membered heteroaryl groups are indol-1-yl, indol-2-yl, indol-3-yl, indol-4-yl, indol-5-yl, Indole-6-yl, indole-7-yl, benzimidazol-1-yl, benzimidazol-2-yl, benzimidazol-4-yl, benzimidazol-5-yl, indazole-1 -Yl, indazol-3-yl, indazol-4-yl, indazol-5-yl, indazol-6-yl, indazol-7-yl, indazol-2-yl, 1-benzofuran 2-yl, 1-benzofuran-3-yl, 1-benzofuran-4-yl, 1-benzofuran-5-yl, 1-benzofuran-6-yl, 1-benzofuran -7-yl, 1-benzothiophen-2-yl, 1-benzothiophen-3-yl, 1-benzothiophen-4-yl, 1-benzothiophen-5-yl, 1-benzothiophene -6-yl, 1-benzothiophen-7-yl, 1,3-benzothiazol-2-yl, 1,3-benzothiazol-4-yl, 1,3-benzothiazol-5-yl , 1,3-benzothiazole-6-yl, 1,3-benzothiazole-7-yl, 1,3-benzo
Figure TW201945344A_D0030
Azol-2-yl, 1,3-benzo
Figure TW201945344A_D0031
Azole-4-yl, 1,3-benzo
Figure TW201945344A_D0032
Azol-5-yl, 1,3-benzo
Figure TW201945344A_D0033
Azole-6-yl and 1,3-benzo
Figure TW201945344A_D0034
Azole-7-yl. Examples of benzo-fused 6-membered heteroaryl groups are quinolin-2-yl, quinolin-3-yl, quinolin-4-yl, quinolin-5-yl, quinolin-6-yl, Quinolin-7-yl, quinolin-8-yl, isoquinolin-1-yl, isoquinolin-3-yl, isoquinolin-4-yl, isoquinolin-5-yl, isoquinolin- 6-yl, isoquinolin-7-yl and isoquinolin-8-yl. Further examples of 5- or 6-membered heteroaryl groups as part of the bicyclic system are 1,2,3,4-tetrahydroquinolin-1-yl, 1,2,3,4-tetrahydroquinoline-2- 1,2,3,4-tetrahydroquinoline-7-yl, 1,2,3,4-tetrahydroquinoline-8-yl, 1,2,3,4-tetrahydroisoquinoline- 1-yl, 1,2,3,4-tetrahydroisoquinolin-2-yl, 1,2,3,4-tetrahydroisoquinolin-5-yl, 1,2,3,4-tetrahydro Isoquinoline-6-yl and 1,2,3,4-tetrahydroisoquinoline-7-yl. Unless otherwise defined elsewhere, this definition also applies to heteroaryl groups that are part of a combined substituent, such as heteroaralkyl.

雜環基：三-至七-員、飽和或部分不飽和雜環，其含有至少一個，若適當的話至多四個獨立地由N、O、S、S(=O)、S(=O)2和二-(C1-C4)烷基矽基組成之群中選出的雜原子及/或雜基團，該基團可為苯并稠合環。與上級通式結構之鍵結可經由環碳原子或，若可能的話，經由雜環基的環氮原子來進行。在此意義上飽和雜環為，例如(但不限於)氧

Figure TW201945344A_D0035
基(oxiranyl)、氮丙啶基(aziridinyl)、四氫呋喃-2-基、四氫呋喃-3-基、四氫噻吩-2-基、四氫噻吩-3-基、吡咯啶-2-基、吡咯啶-3-基、異
Figure TW201945344A_D0036
唑啶-3-基、異
Figure TW201945344A_D0037
唑啶-4-基、異
Figure TW201945344A_D0038
唑啶-5-基、異噻唑啶-3-基、異噻唑啶-4-基、異噻唑啶-5-基、吡唑啶-3-基、吡唑啶-4-基、吡唑啶-5-基、
Figure TW201945344A_D0039
唑啶-2-基、
Figure TW201945344A_D0040
唑啶-4-基、
Figure TW201945344A_D0041
唑啶-5-基、噻唑啶-2-基、噻唑啶-4-基、噻唑啶-5-基、咪唑啶-2-基、咪唑啶-4-基、1,2,4-
Figure TW201945344A_D0042
二唑啶-3-基、1,2,4-
Figure TW201945344A_D0043
二唑啶-5-基、1,3,4-
Figure TW201945344A_D0044
二唑啶-2-基、1,2,4-噻二唑啶-3-基、1,2,4-噻二唑啶-5-基、1,3,4-噻二唑啶-2-基、1,2,4-三唑啶-3-基、1,3,4-三唑啶-2-基、哌啶-2-基、哌啶-3-基、哌啶-4-基、1,3-二氧六圜基-5-基、四氫吡喃-2-基、四氫吡喃-4-基、四氫噻吩-2-基、六氫嗒
Figure TW201945344A_D0045
-3-基、六氫嗒
Figure TW201945344A_D0046
-4-基、六氫嘧啶-2-基、六氫嘧啶-4-基、六氫嘧啶-5-基、哌
Figure TW201945344A_D0047
-2-基、1,3,5-六氫三
Figure TW201945344A_D0048
-2-基和1,2,4-六氫三
Figure TW201945344A_D0049
-3-基。在此意義上部分不飽和雜環基基團為，例如(但不限於)2,3-二氫呋喃-2-基、2,3-二氫呋喃-3-基、2,4-二氫呋喃-2-基、2,4-二氫呋喃-3-基、2,3-二氫噻吩-2-基、2,3-二氫噻吩-3-基、2,4-二氫噻吩-2-基、2,4-二氫噻吩-3-基、2-吡咯啉-2-基、2-吡咯啉-3-基、3-吡咯啉-2-基、3-吡咯啉-3-基、2-異
Figure TW201945344A_D0050
唑啉-3-基、3-異
Figure TW201945344A_D0051
唑啉-3-基、4-異
Figure TW201945344A_D0052
唑啉-3-基、2-異
Figure TW201945344A_D0053
唑啉-4-基、3-異
Figure TW201945344A_D0054
唑啉-4-基、4-異
Figure TW201945344A_D0055
唑啉-4-基、2-異
Figure TW201945344A_D0056
唑啉-5-基、3-異
Figure TW201945344A_D0057
唑啉-5-基、4-異
Figure TW201945344A_D0058
唑啉-5-基、2-異噻唑啉-3-基、3-異噻唑啉-3-基、4-異噻唑啉-3-基、2-異噻唑啉-4-基、3-異噻唑啉-4-基、4-異噻唑啉-4-基、2-異噻唑啉-5-基、3-異噻唑啉-5-基、4-異噻唑啉-5-基、2,3-二氫吡唑--1-基、2,3- 二氫吡唑--2-基、2,3-二氫吡唑-3-基、2,3-二氫吡唑-4-基、2,3-二氫吡唑-5-基、3,4-二氫吡唑--1-基、3,4-二氫吡唑--3-基、3,4-二氫吡唑-4-基、3,4-二氫吡唑-5-基、4,5-二氫吡唑-1-基、4,5-二氫吡唑-3-基、4,5-二氫吡唑-4-基、4,5-二氫吡唑-5-基、2,3-二氫
Figure TW201945344A_D0059
唑-2-基、2,3-二氫
Figure TW201945344A_D0060
唑-3-基、2,3-二氫
Figure TW201945344A_D0061
唑-4-基、2,3-二氫
Figure TW201945344A_D0062
唑-5-基、3,4-二氫
Figure TW201945344A_D0063
唑-2-基、3,4-二氫
Figure TW201945344A_D0064
唑-3-基、3,4-二氫
Figure TW201945344A_D0065
唑-4-基、3,4-二氫
Figure TW201945344A_D0066
唑-5-基、3,4-二氫
Figure TW201945344A_D0067
唑-2-基、3,4-二氫
Figure TW201945344A_D0068
唑-3-基、3,4-二氫
Figure TW201945344A_D0069
唑-4-基。苯并稠合雜環基團的實例有吲哚啉-1-基、吲哚啉-2-基、吲哚啉-3-基、異吲哚啉-1-基、異吲哚啉-2-基、2,3-二氫苯并呋喃-2-基和2,3-二氫苯并呋喃-3-基。除非他處另有定義，否則此定義亦適用於作為組合取代基之部分的雜環基，例如雜環基烷基。 Heterocyclyl: a three- to seven-membered, saturated or partially unsaturated heterocyclic ring containing at least one, and if appropriate, up to four, independently of N, O, S, S (= O), S (= O) Heteroatoms and / or heterogroups selected from the group consisting of 2 and di- (C 1 -C 4 ) alkylsilyl groups, which may be benzo-fused rings. The bonding to the higher-level structure can be carried out via a ring carbon atom or, if possible, via a ring nitrogen atom of a heterocyclic group. A saturated heterocycle in this sense is , for example, but not limited to, oxygen
Figure TW201945344A_D0035
Oxiranyl, aziridinyl, tetrahydrofuran-2-yl, tetrahydrofuran-3-yl, tetrahydrothiophen-2-yl, tetrahydrothiophen-3-yl, pyrrolidin-2-yl, pyrrolidine -3-yl, iso
Figure TW201945344A_D0036
Oxazidin-3-yl, iso
Figure TW201945344A_D0037
Oxazol-4-yl, iso
Figure TW201945344A_D0038
Amidazol-5-yl, isothiazolidine-3-yl, isothiazolidine-4-yl, isothiazolidine-5-yl, pyrazolidine-3-yl, pyrazolidine-4-yl, pyrazidine -5-base,
Figure TW201945344A_D0039
Oxazidin-2-yl,
Figure TW201945344A_D0040
Oxazol-4-yl,
Figure TW201945344A_D0041
Amidazol-5-yl, thiazolidine-2-yl, thiazolidine-4-yl, thiazolidine-5-yl, imidazol-2-yl, imidazol-4-yl, 1,2,4-
Figure TW201945344A_D0042
Diazolidin-3-yl, 1,2,4-
Figure TW201945344A_D0043
Oxazolidin-5-yl, 1,3,4-
Figure TW201945344A_D0044
Oxadiazin-2-yl, 1,2,4-thiadiazolidine-3-yl, 1,2,4-thiadiazolidine-5-yl, 1,3,4-thiadiazolidine-2 -Yl, 1,2,4-triazolidin-3-yl, 1,3,4-triazolidin-2-yl, piperidin-2-yl, piperidin-3-yl, piperidin-4- Group, 1,3-dioxohexanyl-5-yl, tetrahydropyran-2-yl, tetrahydropyran-4-yl, tetrahydrothiophen-2-yl, hexahydro
Figure TW201945344A_D0045
-3-yl, hexahydro
Figure TW201945344A_D0046
-4-yl, hexahydropyrimidin-2-yl, hexahydropyrimidin-4-yl, hexahydropyrimidin-5-yl, piperidine
Figure TW201945344A_D0047
-2-yl, 1,3,5-hexahydrotris
Figure TW201945344A_D0048
-2-yl and 1,2,4-hexahydrotri
Figure TW201945344A_D0049
-3-yl. In this sense, partially unsaturated heterocyclyl groups are, for example, but not limited to, 2,3-dihydrofuran-2-yl, 2,3-dihydrofuran-3-yl, 2,4-dihydro Furan-2-yl, 2,4-dihydrofuran-3-yl, 2,3-dihydrothiophen-2-yl, 2,3-dihydrothiophen-3-yl, 2,4-dihydrothiophene- 2-yl, 2,4-dihydrothiophen-3-yl, 2-pyrrolidin-2-yl, 2-pyrrolidin-3-yl, 3-pyrrolidin-2-yl, 3-pyrrolidin-3- Base, 2-iso
Figure TW201945344A_D0050
Oxazolin-3-yl, 3-iso
Figure TW201945344A_D0051
Oxazolin-3-yl, 4-iso
Figure TW201945344A_D0052
Oxazolin-3-yl, 2-iso
Figure TW201945344A_D0053
Oxazolin-4-yl, 3-iso
Figure TW201945344A_D0054
Oxazolin-4-yl, 4-iso
Figure TW201945344A_D0055
Oxazolin-4-yl, 2-iso
Figure TW201945344A_D0056
Oxazolin-5-yl, 3-iso
Figure TW201945344A_D0057
Oxazolin-5-yl, 4-iso
Figure TW201945344A_D0058
Oxazolin-5-yl, 2-isothiazolin-3-yl, 3-isothiazolin-3-yl, 4-isothiazolin-3-yl, 2-isothiazolin-4-yl, 3-iso Thiazolin-4-yl, 4-isothiazolin-4-yl, 2-isothiazolin-5-yl, 3-isothiazolin-5-yl, 4-isothiazolin-5-yl, 2,3 -Dihydropyrazol-1-yl, 2,3-dihydropyrazol-2-yl, 2,3-dihydropyrazol-3-yl, 2,3-dihydropyrazol-4-yl , 2,3-dihydropyrazol-5-yl, 3,4-dihydropyrazol-1-yl, 3,4-dihydropyrazol-3-yl, 3,4-dihydropyrazole 4-yl, 3,4-dihydropyrazol-5-yl, 4,5-dihydropyrazol-1-yl, 4,5-dihydropyrazol-3-yl, 4,5-dihydro Pyrazol-4-yl, 4,5-dihydropyrazol-5-yl, 2,3-dihydro
Figure TW201945344A_D0059
Azol-2-yl, 2,3-dihydro
Figure TW201945344A_D0060
Azol-3-yl, 2,3-dihydro
Figure TW201945344A_D0061
Azole-4-yl, 2,3-dihydro
Figure TW201945344A_D0062
Azol-5-yl, 3,4-dihydro
Figure TW201945344A_D0063
Azol-2-yl, 3,4-dihydro
Figure TW201945344A_D0064
Azol-3-yl, 3,4-dihydro
Figure TW201945344A_D0065
Azole-4-yl, 3,4-dihydro
Figure TW201945344A_D0066
Azol-5-yl, 3,4-dihydro
Figure TW201945344A_D0067
Azol-2-yl, 3,4-dihydro
Figure TW201945344A_D0068
Azol-3-yl, 3,4-dihydro
Figure TW201945344A_D0069
Azole-4-yl. Examples of benzo-fused heterocyclic groups are indololin-1-yl, indololin-2-yl, indololin-3-yl, isoindololin-1-yl, isoindolin-2 -Yl, 2,3-dihydrobenzofuran-2-yl and 2,3-dihydrobenzofuran-3-yl. Unless otherwise defined elsewhere, this definition also applies to heterocyclyls that are part of a combination of substituents, such as heterocyclylalkyl.

側氧基係代表雙鍵氧原子。 The pendant oxygen system represents a double bond oxygen atom.

硫酮基(thiooxo)係代表雙鍵硫原子。 The thiooxo group represents a double bond sulfur atom.

視需要經取代基團可為單-或多取代，其中在多取代情況下之取代基可相同或不同。 The substituted group may be mono- or poly-substituted, if necessary, wherein the substituents in the case of poly-substitution may be the same or different.

不包括在內的為違反自然法則的組合，且熟習本項技術者因此應能以其專業的知識為基準將其排除。例如，不包括具有三或更多鄰接氧原子的環結構。 Excluded are combinations that violate the laws of nature, and those skilled in the art should be able to exclude them based on their professional knowledge. For example, a ring structure having three or more adjacent oxygen atoms is not included.

異構物Isomers

依照取代基的性質，本發明化合物可以不同的立體異構物形式存在。這些立體異構物有，例如鏡像異構物、非對映異構物、構型異構物(atropisomer)或幾何異構物。因此，本發明係涵蓋純的立體異構物及這些異構物之任何混合物。當一化合物可在平衡時以二或更多互變異構物形式存在時，有關藉由一互變異構描述之化合物應視為包括所有的互變異構型。 Depending on the nature of the substituents, the compounds of the invention may exist in different stereoisomeric forms. These stereoisomers are, for example, enantiomers, diastereomers, atropisomers or geometric isomers. Accordingly, the present invention encompasses pure stereoisomers and any mixtures of these isomers. When a compound can exist as two or more tautomers at equilibrium, the compounds described by one tautomer should be considered to include all tautomeric forms.

方法和中間物之說明Description of methods and intermediates

本發明再者係關於製備式(I)化合物，包括式(Ia)、(Ib)和(Ic)之化合物的方法。 The invention further relates to a method for preparing a compound of formula (I), including compounds of formulae (Ia), (Ib) and (Ic).

化合物(I)可藉由各種路徑，以類似先前技術中已知的方法來製得。特言之，藉由調整先前所述用於合成含有對應1,2,4-三唑-類似物之方法 (參見，例如EP-A 251086；WO-A 1989/005581；EP-A 321211；WO-A 1991/012000；Maurin et al.Pharmaceutical Research 1993,10(2),309-12；International Journal of Pharmaceutic 1993,94(1-3),11-14；DE-A 4419812及其內文所引述的參考文獻)，調整WO-A 2016/156290中所揭示的方法及藉由下文以及本申請案實驗部分示意圖所示的合成路徑。除非另有指出，否則Q、R1、R2、R2a、R3、R4和R5具有上文式(I)化合物所給予的意義。這些定義不僅適用於式(I)之最終產物亦同樣適用於所有的中間物。 Compound (I) can be prepared by various routes in a manner similar to that known in the prior art. In particular, the method for synthesizing the corresponding 1,2,4-triazole-analogues by adjusting the previously described method (see, eg, EP-A 251086; WO-A 1989/005581; EP-A 321211; WO -A 1991/012000; Maurin et al. Pharmaceutical Research 1993 , 10 (2), 309-12; International Journal of Pharmaceutic 1993 , 94 (1-3), 11-14; DE-A 4419812 and its content cited in the text References), adjusting the method disclosed in WO-A 2016/156290 and the synthetic route shown below and in the schematic diagram of the experimental part of this application. Unless otherwise indicated, Q, R 1, R 2, R 2a, R 3, R 4 and R 5 have the meanings above with a compound of formula (I) given. These definitions apply not only to the final product of formula (I) but also to all intermediates.

僅就更佳了解下列式(I)化合物之流程圖，其中R2為OH已被指定為化合物(I-OH)。化合物(I-OH)係涵蓋在如上所定義的通式(I)內。 The flow chart of the compound of formula ( I ) below, where R 2 is OH has been designated as compound ( I-OH ), for better understanding only. The compound ( I-OH ) is encompassed within the general formula ( I ) as defined above.

Figure TW201945344A_D0070
Figure TW201945344A_D0070

在流程1之方法中，式(III)的酮，其可根據以前所描述的方法(例如根據WO-A 2016/156290，特言之根據文中所述的方法J至L)，與衍生物(II)反應來製得，其中G係代表鹵素或氫。 In the process of Scheme 1, the ketone of formula (III), which may be (e.g., L J The method according to WO-A 2016/156290, Japanese words in accordance with described herein) according to the method previously described, and derivatives ( II) , wherein G represents halogen or hydrogen.

在G代表氫的情況下，化合物(II)[其製備大部分係使用例如威悌(Wittig)、霍納爾-沃茲沃思-埃蒙斯(Horner-Wadsworth-Emmons)或朱利亞烯化反應(Julia olefination)，由羰基化合物開始來描述]可與金屬化試劑反應，較佳地在無水條件下反應。適合的金屬化試劑可為烷基金屬試劑，例如甲基鋰、正丁基鋰、苯基鋰或異丙基鎂鹵化物或醯胺鹼(例如二異丙基醯 胺鋰或雙(三甲基矽基)醯胺鋰)之溶液，視需要在添加鹽類(例如氯化鋰)的存在下。將得到的有機金屬中間物隨後與酮(III)反應，較佳地在無水條件下反應，得到通式(I-OH)之化合物。 In the case where G represents hydrogen, compound (II) [Its preparation is mostly made using, for example, Wittig, Horner-Wadsworth-Emmons, or Julia alkylation (Julia olefination, described starting with a carbonyl compound) can react with a metallizing agent, preferably under anhydrous conditions. Suitable metallization reagents can be alkyl metal reagents, such as methyl lithium, n-butyl lithium, phenyl lithium, or isopropyl magnesium halides or amidine bases (e.g., lithium diisopropylammonium or bis (trimethyl) A solution of silicon based) lithium amidoamine), if necessary in the presence of added salts (such as lithium chloride). The obtained organometallic intermediate is then reacted with ketone (III) , preferably under anhydrous conditions, to obtain a compound of general formula ( I-OH) .

在G代表鹵素的情況下，化合物(II)[其可從市面上購得或可藉由文獻已知的方法來製備，例如藉由將對應的苯乙烯二溴化，接著如US2009/30238中所述或由Piou & Rovis,J.Am.Chem.Soc. 2014,136(32),11292-11295所述的鹼促化消除]可先與金屬(例如適當的形式(例如金屬粉末或屑)的鋰、鎂或鋅)或與烷基金屬試劑(例如甲基鋰、正丁基鋰、苯基鋰或異丙基鎂鹵化物之溶液，在有添加鹽類或無添加鹽類(例如氯化鋰)下)反應，及隨後與酮(III)反應，視需要在添加鹽類(例如氯化鋰)的存在下反應，較佳地在無水條件下，得到通式(I-OH)化合物。依照羰基基質而定，其可能有利的以例如三烷氧基鋯(IV)或三烷氧基鈦(IV)[參見，例如Weidmann,Seebach,Angew.Chem.Int.Ed. 1983,22(1),31-45]，三氯化鈰(III)[參見，例如Imamoto et al.,J.Am.Chem.Soc. 1989,111(12),pp 4392-4398]，三氯化鑭(III)[參見，例如Krasovskiy et al.,Angew.Chem.Int.Ed. 2006,45(3),497-500]，氯化鎂(II)[參見，例如Metzger et al.,Angew.Chem.Int.Ed. 2010,49(27),4665-4668]，氯化鋅(II)[參見，例如Hatano et al.,J.Org.Chem. 2010,75(15),5008-5016]，或氯化錳(II)[參見，例如Quinio et al.,Synlett 2015,26(04),514-518]，進行中間物轉金屬步驟。 In the case where G represents halogen, the compound (II) [which is commercially available or can be prepared by methods known in the literature, for example by dibromizing the corresponding styrene, followed by US2009 / 30238 Alkali-catalyzed elimination as described or described by Piou & Rovis, J. Am. Chem. Soc. 2014 , 136 (32), 11292-11295] may be preceded with a metal (e.g., a suitable form (e.g., metal powder or shavings) Lithium, magnesium or zinc) or a solution with an alkyl metal reagent (e.g. methyllithium, n-butyllithium, phenyllithium or isopropylmagnesium halide), with or without added salts (e.g. chlorine Lithium)) and subsequent reaction with ketone (III) , if necessary in the presence of added salts (such as lithium chloride), preferably under anhydrous conditions, to obtain compounds of general formula ( I-OH) . Depending on the carbonyl matrix, it may be advantageous, for example, to give trialkoxyzirconium (IV) or trialkoxide titanium (IV) [see, for example, Weidmann, Seebach, Angew. Chem. Int. Ed. 1983 , 22 (1 ), 31-45], cerium (III) trichloride [see, for example, Imamoto et al. , J. Am. Chem. Soc. 1989 , 111 (12), pp 4392-4398], lanthanum trichloride (III ) [See, eg, Krasovskiy et al. , Angew. Chem. Int. Ed. 2006 , 45 (3), 497-500], magnesium (II) chloride [see, eg, Metzger et al. , Angew . Chem . Int . Ed 2010, 49 (27), 4665-4668], zinc (II) [see, e.g. Hatano et al., J.Org.Chem. 2010 , 75 (15), 5008-5016], or manganese chloride (II) [See, for example, Quinio et al. , Synlett 2015 , 26 (04), 514-518], performing the intermediate to metal step.

較佳地，此反應係在溶劑的存在下進行。關於溶劑，可使用所有在反應條件下為惰性的常見溶劑，例如醚類(例如乙醚、四氫呋喃、2-甲基四氫呋喃)、二氯甲烷或其混合物，而反應可在二或更多這些溶劑的混合物中進行。 Preferably, this reaction is performed in the presence of a solvent. As for the solvent, all common solvents that are inert under the reaction conditions, such as ethers (e.g., diethyl ether, tetrahydrofuran, 2-methyltetrahydrofuran), dichloromethane, or mixtures thereof can be used, and the reaction can be performed in two or more of these solvents. Performed in the mixture.

反應較佳地係在介於-78℃至溶劑回流溫度之間的溫度下進行，更佳地介於-50℃至25℃之間。 The reaction is preferably carried out at a temperature between -78 ° C and the reflux temperature of the solvent, more preferably between -50 ° C and 25 ° C.

方法B(流程2)：Method B (flow 2):

Figure TW201945344A_D0071
Figure TW201945344A_D0071

在流程2之方法中，式(IV)之環氧化物，其可根據以前所述的方法(例如根據EP-A 251086；WO-A 1989/005581；EP-A 321211；WO-A 1991/012000；DE-A4419812)與咪唑(V)反應，其可從市面上購得或可藉由文獻中所述的方法，視需要在鹼的存在下，例如碳酸鉀及/或第三丁醇鉀，視需要在路易士酸的存在下(例如氯化鎂或BF3/Et2O)來製得。或者，亦可使用有機鎂鹼(例如MeMgCl、TMPMgCl或類似物)(參見Org.Lett.,2016,18(1),pp 16-19)。 In the method of Scheme 2, the epoxide of formula ( IV) may be according to the method described previously (e.g. DE-A4419812) reacts with imidazole (V) , which is commercially available or can be described in the literature by methods described in the literature, if necessary in the presence of a base, such as potassium carbonate and / or potassium tert-butoxide, It is optionally prepared in the presence of Lewis acid (for example, magnesium chloride or BF 3 / Et 2 O). Alternatively, organomagnesium bases (such as MeMgCl, TMPMgCl, or the like) can also be used (see Org. Lett. , 2016 , 18 (1), pp 16-19).

較佳地，此反應係在溶劑的存在下進行。關於溶劑，可使用所有在反應條件下為惰性的常見溶劑，例如腈類(例如乙腈、丙腈)或醯胺類(例如DMF、DMAc或NMP)，且反應可在二或更多這些溶劑的混合物中進行。 Preferably, this reaction is performed in the presence of a solvent. As the solvent, all common solvents that are inert under the reaction conditions, such as nitriles (e.g., acetonitrile, propionitrile) or amidines (e.g., DMF, DMAc, or NMP) can be used, and the reaction can be performed in two or more of these solvents. Performed in the mixture.

反應較佳地係在介於-78℃至溶劑回流溫度之間的溫度下進行，更佳地介於25℃至150℃之間。 The reaction is preferably carried out at a temperature between -78 ° C and the reflux temperature of the solvent, more preferably between 25 ° C and 150 ° C.

化合物(I-OH)和化合物(VI)可藉由本項技術中熟知的技術，例如層析來分離。 Compound (I-OH) and compound (VI ) can be separated by a technique well known in the art, such as chromatography.

若無法直接藉由上述路徑製得個別的化合物(I)，則其可藉由其他的式(I)化合物之衍生作用來製備。特言之，式(I-OH)化合物的羥基基團可容易地藉由文獻中所述的方法轉變成其中R2不為OH的對應化合物(I)(參見，例如DE-A 3202604,JP-A 02101067,EP-A 225 739,CN-A 101824002,FR-A 2802772；WO-A 2012/175119,Bioorganic & Medicinal Chemistry Letters,7207-7213,2012；Journal of the American Chemical Society,19358-19361,2012,Journal of Organic Chemistry,9458-9472,2012；Organic Letters,554-557,2013；Journal of the American Chemical Society,15556, 2012)。例如，通用結構(I-OH)之化合物可與烷基鹵化物、二烷基硫酸酯、酸酐、氯酸、磷醯氯、烷基異氰酸酯、胺甲醯氯、氯甲酸酯或亞胺碳酸酯，較佳地在鹼的存在下，得到其中R2不為OH的化合物(I)。 If the individual compound (I) cannot be directly obtained through the above route, it can be prepared by derivatization of other compounds of the formula (I) . In particular, the hydroxyl group of a compound of the formula ( I-OH) can be easily converted into the corresponding compound (I) in which R 2 is not OH by a method described in the literature (see, for example, DE-A 3202604, JP -A 02101067, EP-A 225 739, CN-A 101824002, FR-A 2802772; WO-A 2012/175119, Bioorganic & Medicinal Chemistry Letters, 7207-7213, 2012; Journal of the American Chemical Society, 19358-19361, 2012, Journal of Organic Chemistry, 9458-9472, 2012; Organic Letters, 554-557, 2013; Journal of the American Chemical Society, 15556, 2012). For example, compounds of general structure (I-OH) can be reacted with alkyl halides, dialkyl sulfates, anhydrides, chloric acid, phosphorous chloride, alkyl isocyanates, carbamate chloride, chloroformate, or imine carbonic acid. An ester, preferably in the presence of a base, gives compound (I) in which R 2 is not OH.

通論General theory

根據本發明用於製備式(I)化合物的方法A至B視需要係使用一或多種反應助劑來進行。 Processes A to B for preparing compounds of formula ( I ) according to the invention are carried out, if necessary, using one or more reaction aids.

有用的反應助劑，若適當的話，有無機和有機鹼或酸受質。這些較佳地係包括鹼金屬或鹼土金屬乙酸鹽、碳酸鹽、碳酸氫鹽、氫化物、氫氧化物或烷氧化物，例如乙酸鈉、乙酸鉀或乙酸鈣、醯胺鋰、醯胺鈉、醯胺鉀或醯胺鈣、碳酸鈉、碳酸鉀或碳酸鈣、碳酸氫鈉、碳酸氫鉀或碳酸氫鈣、氫化鋰、氫化鈉、氫化鉀或氫化鈣、氫氧化鋰、氫氧化鈉、氫氧化鉀或氫氧化鈣、正丁基鋰、第二丁基鋰、第三丁基鋰、二異丙基醯胺鋰、雙(三甲基矽基)醯胺鋰、甲醇鈉、乙醇鈉、正-或異丙醇鈉、正-、異-、第二-或第三丁醇鈉或甲醇鉀、乙醇鉀、正-或異丙醇鉀、正-、異-、第二-或第三丁醇鉀；以及鹼性有機氮化合物，例如三甲基胺、三乙基胺、三丙基胺、三丁基胺、乙基二異丙基胺、N,N-二甲基環己基胺、二環己基胺、乙基二環己基胺、N,N-二甲基苯胺、N,N-二甲基苯甲基胺、吡啶、2-甲基-、3-甲基-、4-甲基-、2,4-二甲基-、2,6-二甲基-、3,4-二甲基-和3,5-二甲基吡啶、5-乙基-2-甲基吡啶、4-二甲基胺基吡啶、N-甲基哌啶、1,4-二氮雜雙環[2.2.2]-辛烷(DABCO)、1,5-二氮雜雙環[4.3.0]-壬-5-烯(DBN)或1,8-二氮雜雙環[5.4.0]-十一-7-烯(DBU)。 Useful reaction auxiliaries, if appropriate, are supported by inorganic and organic bases or acids. These preferably include alkali metal or alkaline earth metal acetates, carbonates, bicarbonates, hydrides, hydroxides, or alkoxides, such as sodium acetate, potassium acetate or calcium acetate, lithium ammonium, sodium ammonium, Ammonium potassium or ammonium calcium, sodium carbonate, potassium carbonate or calcium carbonate, sodium bicarbonate, potassium bicarbonate or calcium bicarbonate, lithium hydride, sodium hydride, potassium or calcium hydride, lithium hydroxide, sodium hydroxide, hydrogen Potassium oxide or calcium hydroxide, n-butyllithium, second butyllithium, third butyllithium, lithium diisopropylamide, lithium bis (trimethylsilyl) amide, sodium methoxide, sodium ethoxide, Sodium n- or isopropoxide, n-, iso-, second- or third butanol or potassium methoxide, potassium ethoxide, n- or potassium isopropoxide, n-, iso-, second- or third Potassium butoxide; and basic organic nitrogen compounds such as trimethylamine, triethylamine, tripropylamine, tributylamine, ethyldiisopropylamine, N, N-dimethylcyclohexylamine , Dicyclohexylamine, ethyldicyclohexylamine, N, N-dimethylaniline, N, N-dimethylbenzylamine, pyridine, 2-methyl-, 3-methyl-, 4- Methyl-, 2,4-dimethyl-, 2,6- Dimethyl-, 3,4-dimethyl- and 3,5-dimethylpyridine, 5-ethyl-2-methylpyridine, 4-dimethylaminopyridine, N-methylpiperidine, 1,4-diazabicyclo [2.2.2] -octane (DABCO), 1,5-diazabicyclo [4.3.0] -non-5-ene (DBN) or 1,8-diaza Bicyclic [5.4.0] -undec-7-ene (DBU).

可使用的反應助劑，若適當的話，有無機或有機酸。這些較佳地係包括無機酸，例如氫氟酸、氫氯酸、氫溴酸和氫碘酸、硫酸，磷酸和硝酸，以及酸的鹽類，例如NaHSO4和KHSO4，或有機酸，例如甲酸、碳酸和烷酸，例如乙酸、三氟乙酸、三氯乙酸和丙酸，以及羥基乙酸、硫氰酸、乳酸、琥珀酸、檸檬酸、苯甲酸、肉桂酸、草酸、飽和的或單-或二不飽和C6-C20脂肪酸、烷基硫酸酯、烷基磺酸(具有帶有1-20個碳原子之直鏈或支鏈烷基的磺酸)、芳基磺酸或芳基二磺酸(芳香基如苯基和萘基，其係帶有一個 或兩個磺酸基團)、烷基膦酸(具有帶有1-20個碳原子之直鏈或支鏈烷基的膦酸)、芳基膦酸或芳基二膦酸(芳香基如苯基和萘基，其係帶有一個或兩個膦酸基)，其中烷基或芳基可帶有另外的取代基，例如對甲苯磺酸、水楊酸、對胺基水楊酸、2-苯氧基苯甲酸、2-乙醯氧基苯甲酸。 The reaction aids that can be used are, if appropriate, inorganic or organic acids. These preferably include inorganic acids such as hydrofluoric acid, hydrochloric acid, hydrobromic acid and hydroiodic acid, sulfuric acid, phosphoric acid and nitric acid, and salts of acids such as NaHSO 4 and KHSO 4 , or organic acids such as Formic acid, carbonic acid, and alkanoic acids, such as acetic acid, trifluoroacetic acid, trichloroacetic acid, and propionic acid, and glycolic acid, thiocyanic acid, lactic acid, succinic acid, citric acid, benzoic acid, cinnamic acid, oxalic acid, saturated or mono- Or diunsaturated C 6 -C 20 fatty acids, alkyl sulfates, alkylsulfonic acids (sulfonic acids with straight or branched chain alkyl groups having 1-20 carbon atoms), arylsulfonic acids or aryl groups Disulfonic acid (aromatic groups such as phenyl and naphthyl, which carry one or two sulfonic acid groups), alkylphosphonic acid (having straight or branched chain alkyl groups having 1-20 carbon atoms) Phosphonic acid), arylphosphonic acid, or aryldiphosphonic acid (aromatic groups such as phenyl and naphthyl, which carry one or two phosphonic groups), wherein the alkyl or aryl group may have additional substituents For example, p-toluenesulfonic acid, salicylic acid, p-aminosalicylic acid, 2-phenoxybenzoic acid, 2-ethoxybenzoic acid.

方法A至B係視需要使用一或多種稀釋劑來進行。可使用的稀釋劑實際上為所有惰性有機溶劑。除非上述的方法另有指出，否則這些較佳地係包括脂肪系和芳香系，視需要鹵素化的烴類，例如戊烷、己烷、庚烷、環己烷、石油醚、石油精(benzine)、輕石油(ligroin)、苯、甲苯及二甲苯、二氯甲烷、二氯乙烷、氯仿、四氯化碳、氯苯、鄰-二氯苯，醚類例如乙醚、丁醚和甲基第三丁基醚、乙二醇二甲醚、二甘醇二甲醚、四氫呋喃和二

Figure TW201945344A_D0072
烷，酮類如丙酮，甲基乙基酮，甲基異丙基酮及甲基異丁基酮，酯類例如乙酸甲酯及乙酸乙酯，腈類例如乙腈及丙腈，醯胺類例如二甲基甲醯胺、二甲基乙醯胺和N-甲基吡咯烷酮，以及二甲基亞碸，四亞甲基碸和六甲基磷醯胺及DMPU。 Methods A to B are performed using one or more diluents as needed. Useful diluents are virtually all inert organic solvents. Unless otherwise indicated in the above methods, these preferably include aliphatic and aromatic, and halogenated hydrocarbons as needed, such as pentane, hexane, heptane, cyclohexane, petroleum ether, benzine ), Light petroleum (ligroin), benzene, toluene and xylene, dichloromethane, dichloroethane, chloroform, carbon tetrachloride, chlorobenzene, o-dichlorobenzene, ethers such as ether, butyl ether and methyl Tertiary butyl ether, ethylene glycol dimethyl ether, diglyme, tetrahydrofuran, and
Figure TW201945344A_D0072
Alkanes, ketones such as acetone, methyl ethyl ketone, methyl isopropyl ketone and methyl isobutyl ketone, esters such as methyl acetate and ethyl acetate, nitriles such as acetonitrile and propionitrile, and amines such as Dimethylformamide, dimethylacetamide and N-methylpyrrolidone, as well as dimethylmethylene, tetramethylenepyrene and hexamethylphosphoramidine and DMPU.

在上述的方法中，反應溫度可在相當廣泛的範圍內變化。一般而言，所用的溫度係介於-78℃至250℃間，較佳地介於-78℃至150℃的溫度。 In the methods described above, the reaction temperature can be varied within a relatively wide range. Generally speaking, the temperature used is between -78 ° C and 250 ° C, preferably between -78 ° C and 150 ° C.

反應時間係取決於反應規模和反應溫度而變，但一般係介於數分鐘至48小時之間。 The reaction time varies depending on the scale of the reaction and the reaction temperature, but is generally between a few minutes and 48 hours.

此等方法一般係在標準的壓力下進行。然而，亦可能在升高或降低的壓力下運作。 These methods are generally performed under standard pressure. However, it may also operate under elevated or reduced pressure.

就此等方法的進行，各情況下所需的起始物質一般係以大約等莫耳量來使用。然而，在各情況下亦可能以相對大的過量使用所用的組份之一者。 In order to carry out these methods, the starting materials required in each case are generally used in approximately equimolar amounts. However, it is also possible in each case to use one of the components used in a relatively large excess.

在反應結束後，視需要藉由習用的分離技術從反應混合物中分離化合物。若需要，藉由再結晶或層析將化合物純化。 After completion of the reaction, the compounds are separated from the reaction mixture by conventional separation techniques as necessary. If necessary, the compounds are purified by recrystallization or chromatography.

若適當的話，在A至B的方法中亦可使用起始化合物的鹽類及/或N-氧化物。 If appropriate, salts and / or N-oxides of the starting compounds can also be used in the processes A to B.

鹽類Salt

依照取代基的性質，本發明化合物可以游離化合物及/或農業上可接受的鹽類之形式存在。術語「農業上可接受鹽」係指帶有酸或鹼的本發明化合物，其為農業上可接受的。 Depending on the nature of the substituents, the compounds of the invention may exist as free compounds and / or agriculturally acceptable salts. The term "agriculturally acceptable salt" refers to a compound of the invention with an acid or base, which is agriculturally acceptable.

依照上述定義之取代基的性質，式(I)化合物可具有酸或鹼的性質並可形成鹽類，若適當，帶有無機或有機酸或帶有鹼或帶有金屬離子之惰性鹽類或加合物。若化合物帶有引發鹼性性質之胺基、烷胺基或其他基團，這些化合物可與酸反應得到鹽類，或其可在合成時直接得到鹽類。若化合物帶有引發酸性性質之羥基、羧基或其他基團，則這些化合物可與鹼反應得到鹽類。適合的鹼有，例如，鹼金屬和鹼土金屬，特別是該等鈉、鉀、鎂和鈣的氫氧化物、碳酸鹽、碳酸氫鹽，另外氨、具有(C1-C4)-烷基基團的一級、二級和三級胺，(C1-C4)-烷醇的單-、二-和三烷醇胺以及膽鹼和氯膽鹼。 According to the nature of the substituents as defined above, compounds of formula (I) may have acid or base properties and may form salts, if appropriate, inert salts with inorganic or organic acids or with bases or with metal ions or Adduct. If the compound has an amine group, an alkylamino group or other group that causes basic properties, these compounds can be reacted with an acid to obtain salts, or they can be directly obtained in the synthesis. If the compound has a hydroxyl group, a carboxyl group, or other group that causes acidic properties, these compounds can react with a base to obtain a salt. Suitable bases are, for example, alkali and alkaline earth metals, in particular the hydroxides, carbonates, bicarbonates of such sodium, potassium, magnesium and calcium, in addition ammonia, having (C 1 -C 4 ) -alkyl Primary, secondary and tertiary amines of the group, mono-, di- and trialkanolamines of (C 1 -C 4 ) -alkanol, and choline and chlorocholine.

以此方式所得到的鹽類亦具有殺真菌性質。 The salts obtained in this way also have fungicidal properties.

無機酸的實例有氫鹵酸，例如氫氟酸、氫氯酸、氫溴酸和氫碘酸、硫酸、磷酸和硝酸，及酸鹽，例如NaHSO4和KHSO4。適合的有機酸有，例如甲酸、碳酸和烷酸，如乙酸、三氟乙酸、三氯乙酸和丙酸，及羥基乙酸、硫氰酸、乳酸、琥珀酸、檸檬酸、苯甲酸、肉桂酸、馬來酸、延胡索酸、酒石酸、山梨酸、草酸、烷基磺酸(具有1至20個碳原子之直鏈或支鏈烷基的磺酸)、芳基磺酸或芳基二磺酸(芳香基，例如苯基和萘基，其係帶有一個或兩個磺酸基團)、烷基膦酸(具有1至20個碳原子之直鏈或支鏈烷基的膦酸)、芳基膦酸或芳基二膦酸(芳香基，例如苯基和萘基，其係帶有一個或兩個膦酸基)，其中烷基或芳基可帶有另外的取代基，例如對甲苯磺酸、1,5-萘二磺酸、水楊酸、對胺基水楊酸、2-苯氧基苯甲酸、2-乙醯氧基苯甲酸。 Examples of inorganic acids are hydrohalic acids such as hydrofluoric acid, hydrochloric acid, hydrobromic acid and hydroiodic acid, sulfuric acid, phosphoric acid and nitric acid, and acid salts such as NaHSO 4 and KHSO 4 . Suitable organic acids are, for example, formic acid, carbonic acid and alkanoic acids such as acetic acid, trifluoroacetic acid, trichloroacetic acid and propionic acid, and glycolic acid, thiocyanic acid, lactic acid, succinic acid, citric acid, benzoic acid, cinnamic acid, Maleic acid, fumaric acid, tartaric acid, sorbic acid, oxalic acid, alkylsulfonic acid (sulfonic acid having a linear or branched alkyl group of 1 to 20 carbon atoms), arylsulfonic acid or aryldisulfonic acid (aromatic Radicals, such as phenyl and naphthyl, which carry one or two sulfonic acid groups), alkylphosphonic acids (phosphonic acids of straight or branched chain alkyl groups having 1 to 20 carbon atoms), aryl groups Phosphonic acid or aryl bisphosphonic acid (aromatic groups, such as phenyl and naphthyl, which carry one or two phosphonic acid groups), wherein the alkyl or aryl group may carry additional substituents, such as p-toluenesulfonic acid Acid, 1,5-naphthalenedisulfonic acid, salicylic acid, p-aminosalicylic acid, 2-phenoxybenzoic acid, 2-ethoxybenzoic acid.

適合的金屬離子有特別是第二主族元素的離子，特言之鈣和鎂，第三和第四主族元素的離子，特言之鋁、錫和鉛，以及第一至第八過渡族元素的離子，特言之鉻、錳、鐵、鈷、鎳、銅、鋅和其他。特佳的係給予第四週期元素的金屬離子。本處，金屬可以其可認定的各種價數存在。 Suitable metal ions are ions of the second main group element in particular, calcium and magnesium in particular, ions of the third and fourth main group elements, in particular aluminum, tin and lead, and transition groups 1 to 8 Elemental ions, especially chromium, manganese, iron, cobalt, nickel, copper, zinc and others. A particularly preferred system is a metal ion imparted to the fourth periodic element. Here, metals can exist in various valences that they can identify.

式(I)化合物之酸加成鹽可以簡單的方式藉由習知形成鹽類的方法來製得，例如藉由將式(I)化合物溶於適合的惰性溶劑並加入酸，例如氫氯酸，及以已知的方法，例如過濾分離，若需要，藉由以惰性有機溶劑清洗來純化。 Acid addition salts of compounds of formula (I) can be prepared in a simple manner by conventional methods of forming salts, for example by dissolving a compound of formula (I) in a suitable inert solvent and adding an acid, such as hydrochloric acid , And by known methods, such as filtration and isolation, if necessary, purification by washing with an inert organic solvent.

適合的鹽類之陰離子為該等較佳地衍生自下列酸者：氫鹵酸，例如氫氯酸和氫溴酸，另外磷酸、硝酸和硫酸。 Suitable anions of the salts are those which are preferably derived from the following acids: hydrohalic acids such as hydrochloric acid and hydrobromic acid, in addition phosphoric acid, nitric acid and sulfuric acid.

式(I)化合物的金屬鹽複合物可以簡單的方式藉由習知的方法來製得，例如藉由將金屬鹽溶於醇中，例如乙醇中，並將此溶液加到式(I)化合物中。以已知的方法，例如藉由過濾，可將金屬鹽分離出，及若需要，藉由再結晶純化。 The metal salt complex of the compound of formula (I) can be prepared in a simple manner by conventional methods, for example by dissolving the metal salt in an alcohol, such as ethanol, and adding this solution to the compound of formula (I) in. The metal salt can be isolated by known methods, for example by filtration, and if necessary purified by recrystallization.

就式(I)化合物的鹽類，亦可根據上述方法製備中間物的鹽類。 With regard to the salts of the compound of formula (I), the salts of intermediates can also be prepared according to the method described above.

式(I)化合物或其中間物的N-氧化物可以簡單的方式藉由習知的方法來製得，例如藉由過氧化氫(H2O2)、過氧酸例如過氧硫酸或過氧羧酸，例如間-氯過氧苯甲酸或過氧單硫酸(卡羅酸)之N-氧化作用。 N-oxides of compounds of formula (I) or their intermediates can be prepared in a simple manner by conventional methods, for example by hydrogen peroxide (H 2 O 2 ), peroxy acids such as peroxysulfuric acid or N-oxidation of oxycarboxylic acids such as m-chloroperoxybenzoic acid or peroxymonosulfuric acid (caroic acid).

晶型Crystal form

本發明之化合物可以多種晶型及/或非晶形存在。晶型包括非溶劑化的晶型、溶劑化物和水合物。 The compounds of the invention can exist in a variety of crystalline and / or amorphous forms. Crystal forms include unsolvated crystal forms, solvates, and hydrates.

組成物/調配物Composition / mixture

本發明進一步係關於用於防治有害微生物，較佳地用於防治植物病原性有害真菌的組成物，其係包括至少一種式(I)化合物及至少一種載劑及/或界面活性劑。此等組成物可施用於微生物及/或其棲地。 The invention further relates to a composition for controlling harmful microorganisms, preferably for controlling plant pathogenic harmful fungi, which comprises at least one compound of formula (I) and at least one carrier and / or surfactant. These compositions can be applied to microorganisms and / or their habitat.

載體為固體或液體，天然或合成，有機或無機物質，其一般為惰性的。載劑一般係提升化合物於例如植物、植物部位或種子之施用。適合的固體載劑包括，但不限於，銨鹽、天然礦石粉末，例如高嶺土、黏土、滑石、白堊土、石英、綠坡縷石、蒙脫土和矽藻土，以及合成的礦石粉例如細粉狀矽氧、氧化鋁和矽酸鹽。典型可用於製備顆粒之有用的固體載劑之實例包括，但不限於，粉碎並分級的天然礦石如方解石、大理石、浮石、海泡石和白雲石、合成的無機顆粒和有機粉粉末和有機物質之顆粒，例如 紙、鋸屑、椰子殼、玉米穗軸和煙草桿。適合的液體載劑之實例包括，但不限於，水、有機溶劑及其組合物。適合的溶劑之實例包括極性和非極性有機化學液體，例如芳香和非芳香烴類(例如環己烷、石蠟、烷基苯、二甲苯、甲苯、烷基萘、氯化芳香系和氯化脂肪系烴類，例如氯苯、二氯乙烷和二氯甲烷)、醇類和多元醇類(其視需要亦可經取代、醚化和/或酯化，例如丁醇或甘油)、酮類(例如丙酮、甲基乙基酮、甲基異丁基酮或環己酮)、酯類(包括脂類和油類)和(聚)醚類、未經取代和經取代胺類、醯胺類(例如二甲基甲醯胺)、內醯胺類(如N-烷基吡咯烷酮)和內酯類、碸類和亞碸類(如二甲基亞碸)。載劑亦可為液化氣態增量劑，亦即在標準溫度和標準壓力下為氣態的液體，例如，氣霧劑推進劑，例如鹵化烴類、丁烷、丙烷、氮氣和二氧化碳。載劑的量典型地範圍，以組成物的重量計係從1至99.99%，較佳地5至99.9%，更佳地10至99.5%，及最佳地20至99%。 The carrier is a solid or liquid, natural or synthetic, organic or inorganic substance, which is generally inert. A vehicle is generally an application that enhances the compound to, for example, a plant, plant part, or seed. Suitable solid carriers include, but are not limited to, ammonium salts, natural mineral powders, such as kaolin, clay, talc, chalky soil, quartz, attapulgite, montmorillonite, and diatomaceous earth, and synthetic mineral powders such as fine Powdery silica, alumina and silicate. Examples of useful solid carriers typically useful in the preparation of granules include, but are not limited to, pulverized and classified natural ores such as calcite, marble, pumice, sepiolite and dolomite, synthetic inorganic particles and organic powders, and organic materials. Pellets, such as paper, sawdust, coconut husks, corn cobs, and tobacco rods. Examples of suitable liquid carriers include, but are not limited to, water, organic solvents, and combinations thereof. Examples of suitable solvents include polar and non-polar organic chemical liquids such as aromatic and non-aromatic hydrocarbons (e.g., cyclohexane, paraffin, alkylbenzene, xylene, toluene, alkylnaphthalene, chlorinated aromatics, and chlorinated fatty acids). Hydrocarbons, such as chlorobenzene, dichloroethane, and methylene chloride), alcohols and polyols (which can also be substituted, etherified, and / or esterified if necessary, such as butanol or glycerol), ketones (E.g. acetone, methyl ethyl ketone, methyl isobutyl ketone or cyclohexanone), esters (including lipids and oils) and (poly) ethers, unsubstituted and substituted amines, amidine (E.g. dimethylformamide), lactams (e.g. N-alkylpyrrolidone) and lactones, fluorenes and fluorenes (e.g. dimethylfluorene). The carrier can also be a liquefied gaseous extender, that is, a liquid that is gaseous at standard temperature and pressure, such as aerosol propellants, such as halogenated hydrocarbons, butane, propane, nitrogen, and carbon dioxide. The amount of the carrier typically ranges from 1 to 99.99%, preferably 5 to 99.9%, more preferably 10 to 99.5%, and most preferably 20 to 99% by weight of the composition.

界面活性劑可為離子(陽離子或陰離子)或非離子界面活性劑，例如離子或非離子乳化劑、成泡劑、分散劑、濕潤劑及其任何混合物。適合的界面活性劑之實例包括，但不限於，聚丙烯酸的鹽類、木質素磺酸的鹽類、酚磺酸或者萘磺酸的鹽類、環氧乙烷及/或環氧丙烷與脂肪醇或者與脂肪酸或者與脂肪胺的聚縮合物(聚氧化乙烯脂肪酸酯、聚氧化乙烯脂肪醇醚，例如烷基芳基聚乙二醇醚)、經取代的酚(較佳地烷基酚或芳基酚)、磺基琥珀酸酯的鹽類、牛磺酸衍生物(較佳地烷基牛磺酸酯)、聚乙氧化的醇或酚的膦酸酯、多元醇的脂肪酸酯和含有硫酸鹽、磺酸鹽和磷酸鹽之化合物的衍生物(例如烷基磺酸鹽、烷基硫酸鹽、芳基磺酸鹽)及蛋白質水解物、木質素亞硫酸鹽廢液和甲基纖維素。當本發明化合物及/或該載劑不溶於水且係以水進行施用時，典型地係需要使用界面活性劑。界面活性劑的量，以組成物的重量計，典型地範圍係從5至40%。 The surfactant can be an ionic (cationic or anionic) or non-ionic surfactant, such as an ionic or non-ionic emulsifier, foaming agent, dispersant, humectant, and any mixture thereof. Examples of suitable surfactants include, but are not limited to, salts of polyacrylic acid, salts of ligninsulfonic acid, salts of phenolsulfonic acid or naphthalenesulfonic acid, ethylene oxide and / or propylene oxide and fats Alcohols or polycondensates with fatty acids or with fatty amines (polyoxyethylene fatty acid esters, polyoxyethylene fatty alcohol ethers, such as alkylaryl polyethylene glycol ethers), substituted phenols (preferably alkylphenols) Or arylphenols), salts of sulfosuccinates, taurine derivatives (preferably alkyl taurates), polyethoxylated alcohols or phosphonates of phenols, fatty acid esters of polyols And derivatives of compounds containing sulfates, sulfonates, and phosphates (e.g., alkyl sulfonates, alkyl sulfates, aryl sulfonates) and protein hydrolysates, lignin sulfite waste, and methyl Cellulose. When the compounds of the present invention and / or the vehicle are insoluble in water and are applied in water, a surfactant is typically required. The amount of surfactant, typically based on the weight of the composition, ranges from 5 to 40%.

組成物可包括至少一種其他適合的助劑。 The composition may include at least one other suitable adjuvant.

其他適合的助劑之實例包括防水劑、乾燥劑、結著劑(黏附劑、增黏劑、固著劑，例如羧甲基纖維素、粉末、顆粒和乳膠形式的天然和合成聚合物，例如阿拉伯膠、聚乙烯醇和聚乙酸乙烯酯、天然的磷脂質，例 如腦磷脂和卵磷脂以及合成的磷脂質、聚乙烯吡咯酮和泰勒膠(tylose))、增稠劑、安定劑(例如冷安定劑、防腐劑、抗氧化劑、光安定劑或其他增進化學及/或物理安定性的試劑)、染劑或色素(例如無機色素，例如氧化鐵、氧化鈦和普魯士藍；有機染劑，例如茜素、偶氮和金屬酞青素染劑、消泡劑(例如，聚矽氧消泡劑和硬脂酸鎂)、防腐劑(例如雙氯酚和苯甲醇半縮甲醛)、二次增稠劑(纖維素衍生物、丙烯酸衍生物、黃原膠、修飾黏土和細粉狀矽氧)、黏著劑、吉貝素和加工助劑、礦物油和植物油、芳香劑、蠟、營養素(包括微量營養素，例如鐵、錳、硼、銅、鈷、鉬和鋅的鹽類)、保護膠體、觸變物質、滲透劑、螯合劑和配位劑。 Examples of other suitable auxiliaries include waterproofing agents, desiccants, binding agents (adhesives, tackifiers, fixing agents, such as carboxymethyl cellulose, powders, granules, and natural and synthetic polymers in the form of latex, such as Gum arabic, polyvinyl alcohol and polyvinyl acetate, natural phospholipids such as cerebrolipid and lecithin and synthetic phospholipids, polyvinylpyrrolidone and tylose), thickeners, stabilizers (e.g., cold stabilization) Agents, preservatives, antioxidants, light stabilizers or other agents that enhance chemical and / or physical stability), dyes or pigments (e.g. inorganic pigments, such as iron oxide, titanium oxide and Prussian blue; organic dyes, such as alizarin Pigments, azo and metal phthalocyanin dyes, defoamers (e.g. polysiloxane defoamers and magnesium stearate), preservatives (e.g. bischlorophenol and benzyl alcohol hemiformal), secondary thickening Agents (cellulose derivatives, acrylic acid derivatives, xanthan gum, modified clay and fine powdered silica), adhesives, gebetin and processing aids, mineral and vegetable oils, fragrances, waxes, nutrients (including trace amounts Nutrients such as iron, manganese, boron , Salts of copper, cobalt, molybdenum and zinc), protective colloids, thixotropic substances, penetrants, chelating agents and complexing agents.

助劑之選擇係與本發明化合物之所欲的施用模式及/或物理性質相關。再者，助劑可經選擇用以賦予組成物或從其所製備的使用形式特定的性質(技術、物理及/或生物性質)。助劑之選擇可針對化合物特定需求量身訂製。 The choice of adjuvant is related to the desired mode of application and / or physical properties of the compounds of the invention. Furthermore, the auxiliaries may be selected to impart specific properties (technical, physical and / or biological properties) to the composition or the use forms prepared therefrom. The choice of auxiliaries can be tailored to the specific needs of the compound.

本發明之組成物可為任何習用的形式，例如溶液(例如水溶液)、乳劑、可濕性粉劑、水基和油基懸浮劑、粉劑、粉塵劑、糊劑、可溶性粉劑、可溶性粒劑、佈施用之粒劑、濃縮懸浮乳劑、含浸有本發明化合物之天然或合成產品、肥料以及聚合物中的微膠囊化。本發明之化合物可以懸浮、乳化或溶解的形式存在。 The composition of the present invention may be in any conventional form, such as a solution (e.g., an aqueous solution), an emulsion, a wettable powder, a water-based and an oil-based suspension, a powder, a dust, a paste, a soluble powder, a soluble granule, a spray The granules used, concentrated suspension emulsions, natural or synthetic products impregnated with the compounds of the invention, fertilizers and microencapsulation in polymers. The compounds of the invention may exist in suspended, emulsified or dissolved form.

本發明組成物可以立即可用的調配物形式提供給終端使用者，亦即組成物可藉由適當的裝置，例如噴灑或噴粉裝置直接施用於植物或種子。或者，組成物可以濃縮物之形式提供給終端使用者，其在使用前必須稀釋，較佳地以水稀釋。 The composition of the present invention can be provided to the end user in the form of a ready-to-use formulation, that is, the composition can be directly applied to plants or seeds by a suitable device, such as a spraying or dusting device. Alternatively, the composition may be provided to the end user in the form of a concentrate, which must be diluted before use, preferably with water.

本發明組成物可以習知的方法，例如藉由將本發明化合物與一或多種例如上文中所揭示的適合助劑混合，加以製備。 The composition of the present invention can be prepared in a conventional manner, for example, by mixing a compound of the present invention with one or more suitable adjuvants such as those disclosed above.

本發明組成物一般含有0.01至99%重量比，0.05至98%重量比，較佳地0.1至95%重量比，更佳地0.5至90%重量比，最佳地1至80%重量比的本發明化合物。本發明組成物可能包括二或更多本發明化合物。在此情況下，所述的範圍係指本發明化合物的總量。 The composition of the present invention generally contains 0.01 to 99% by weight, 0.05 to 98% by weight, preferably 0.1 to 95% by weight, more preferably 0.5 to 90% by weight, and most preferably 1 to 80% by weight. Compounds of the invention. Compositions of the invention may include two or more compounds of the invention. In this case, the range refers to the total amount of the compound of the present invention.

混合物/組合物Mixtures / compositions

本發明化合物和組成物可與其他的活性成份混合，如殺真菌劑、殺細菌劑、殺蟎劑、殺線蟲劑、殺蟲劑、除草劑、肥料、生長調節劑、安全劑或訊息化合物。此項可擴大活性譜效或防止抗藥性發生。已知的殺真菌劑、殺蟲劑、殺蟎劑、殺線蟲劑和殺細菌劑係揭示於第17版的Pesticide Manual中。 The compounds and compositions of the present invention can be mixed with other active ingredients, such as fungicides, bactericides, acaricides, nematicides, insecticides, herbicides, fertilizers, growth regulators, safeners or information compounds. This item can expand the spectrum of activity or prevent drug resistance from occurring. Known fungicides, insecticides, acaricides, nematicides and bactericides are disclosed in the 17th edition of the Pesticide Manual.

可與本發明化合物和組成物混合的特佳殺真菌劑之實例有： Examples of particularly preferred fungicides that can be mixed with the compounds and compositions of the present invention are:

1)麥角固醇生物合成抑制劑，例如(1.001)環克座(cyproconazole)、(1.002)待克利(difenoconazole)、(1.003)依普克敏(epoxiconazole)、(1.004)環醯菌胺(fenhexamid)、(1.005)苯鏽啶(fenpropidin)、(1.006)芬普福(fenpropimorph)、(1.007)胺苯吡菌酮(fenpyrazamine)、(1.008)氟喹唑(fluquinconazole)、(1.009)護汰芬(flutriafol)、(1.010)依滅列(imazalil)、(1.011)抑黴唑硫酸鹽(imazalil sulfate)、(1.012)種菌唑(ipconazole)、(1.013)滅特座(metconazole)、(1.014)邁克尼(myclobutanil)、(1.015)巴克素(paclobutrazol)、(1.016)撲克拉(prochloraz)、(1.017)普克利(propiconazole)、(1.018)丙硫菌唑(prothioconazole)、(1.019)啶菌

Figure TW201945344A_D0073
唑(pyrisoxazole)、(1.020)螺環菌胺(spiroxamine)、(1.021)得克利(tebuconazole)、(1.022)四克利(tetraconazole)、(1.023)三泰隆(triadimenol)、(1.024)十三嗎啉(tridemorph)、(1.025)滅菌唑(triticonazole)、(1.026)(1R,2S,5S)-5-(4-氯苯甲基)-2-(氯甲基)-2-甲基-1-(1H-1,2,4-三唑-1-基甲基)環戊醇、(1.027)(1S,2R,5R)-5-(4-氯苯甲基)-2-(氯甲基)-2-甲基-1-(1H-1,2,4-三唑-1-基甲基)環戊醇、(1.028)(2R)-2-(1-氯環丙基)-4-[(1R)-2,2-二氯環丙基]-1-(1H-1,2,4-三唑-1-基)丁-2-醇、(1.029)(2R)-2-(1-氯環丙基)-4-[(1S)-2,2-二氯環丙基]-1-(1H-1,2,4-三唑-1-基)丁-2-醇、(1.030)(2R)-2-[4-(4-氯苯氧基)-2-(三氟甲基)苯基]-1-(1H-1,2,4-三唑-1-基)丙-2-醇、(1.031)(2S)-2-(1-氯環丙基)-4-[(1R)-2,2-二氯環丙基]-1-(1H-1,2,4-三唑-1-基)丁-2-醇、(1.032)(2S)-2-(1-氯環丙基)-4-[(1S)-2,2-二氯環丙基]-1-(1H-1,2,4-三唑-1-基)丁-2-醇、(1.033)(2S)-2-[4-(4-氯苯氧基)-2-(三氟甲基)苯基]-1-(1H-1,2,4-三唑-1-基)丙-2-醇、(1.034)(R)-[3-(4-氯-2-氟苯基)-5-(2,4-二氟苯基)-1,2-
Figure TW201945344A_D0074
唑-4-基](吡啶 -3-基)甲醇、(1.035)(S)-[3-(4-氯-2-氟苯基)-5-(2,4-二氟苯基)-1,2-
Figure TW201945344A_D0075
唑-4-基](吡啶-3-基)甲醇、(1.036)[3-(4-氯-2-氟苯基)-5-(2,4-二氟苯基)-1,2-
Figure TW201945344A_D0076
唑-4-基](吡啶-3-基)甲醇、(1.037)1-({(2R,4S)-2-[2-氯-4-(4-氯苯氧基)苯基]-4-甲基-1,3-二氧戊環-2-基}甲基)-1H-1,2,4-三唑、(1.038)1-({(2S,4S)-2-[2-氯-4-(4-氯苯氧基)苯基]-4-甲基-1,3-二氧戊環-2-基}甲基)-1H-1,2,4-三唑、(1.039)1-{[3-(2-氯苯基)-2-(2,4-二氟苯基)氧
Figure TW201945344A_D0077
-2-基]甲基}-1H-1,2,4-三唑-5-基硫氰酸酯、(1.040)1-{[rel(2R,3R)-3-(2-氯苯基)-2-(2,4-二氟苯基)氧
Figure TW201945344A_D0078
-2-基]甲基}-1H-1,2,4-三唑-5-基硫氰酸酯、(1.041)1-{[rel(2R,3S)-3-(2-氯苯基)-2-(2,4-二氟苯基)氧
Figure TW201945344A_D0079
-2-基]甲基}-1H-1,2,4-三唑-5-基硫氰酸酯、(1.042)2-[(2R,4R,5R)-1-(2,4-二氯苯基)-5-羥基-2,6,6-三甲基庚-4-基]-2,4-二氫-3H-1,2,4-三唑-3-硫酮、(1.043)2-[(2R,4R,5S)-1-(2,4-二氯苯基)-5-羥基-2,6,6-三甲基庚-4-基]-2,4-二氫-3H-1,2,4-三唑-3-硫酮、(1.044)2-[(2R,4S,5R)-1-(2,4-二氯苯基)-5-羥基-2,6,6-三甲基庚-4-基]-2,4-二氫-3H-1,2,4-三唑-3-硫酮、(1.045)2-[(2R,4S,5S)-1-(2,4-二氯苯基)-5-羥基-2,6,6-三甲基庚-4-基]-2,4-二氫-3H-1,2,4-三唑-3-硫酮、(1.046)2-[(2S,4R,5R)-1-(2,4-二氯苯基)-5-羥基-2,6,6-三甲基庚-4-基]-2,4-二氫-3H-1,2,4-三唑-3-硫酮、(1.047)2-[(2S,4R,5S)-1-(2,4-二氯苯基)-5-羥基-2,6,6-三甲基庚-4-基]-2,4-二氫-3H-1,2,4-三唑-3-硫酮、(1.048)2-[(2S,4S,5R)-1-(2,4-二氯苯基)-5-羥基-2,6,6-三甲基庚-4-基]-2,4-二氫-3H-1,2,4-三唑-3-硫酮、(1.049)2-[(2S,4S,5S)-1-(2,4-二氯苯基)-5-羥基-2,6,6-三甲基庚-4-基]-2,4-二氫-3H-1,2,4-三唑-3-硫酮、(1.050)2-[1-(2,4-二氯苯基)-5-羥基-2,6,6-三甲基庚-4-基]-2,4-二氫-3H-1,2,4-三唑-3-硫酮、(1.051)2-[2-氯-4-(2,4-二氯苯氧基)苯基]-1-(1H-1,2,4-三唑-1-基)丙-2-醇、(1.052)2-[2-氯-4-(4-氯苯氧基)苯基]-1-(1H-1,2,4-三唑-1-基)丁-2-醇、(1.053)2-[4-(4-氯苯氧基)-2-(三氟甲基)苯基]-1-(1H-1,2,4-三唑-1-基)丁-2-醇、(1.054)2-[4-(4-氯苯氧基)-2-(三氟甲基)苯基]-1-(1H-1,2,4-三唑-1-基)戊-2-醇、(1.055)2-[4-(4-氯苯氧基)-2-(三氟甲基)苯基]-1-(1H-1,2,4-三唑-1-基)丙-2-醇、(1.056)2-{[3-(2-氯苯基)-2-(2,4-二氟苯基)氧
Figure TW201945344A_D0080
-2-基]甲基}-2,4-二氫-3H-1,2,4-三唑 -3-硫酮、(1.057)2-{[rel(2R,3R)-3-(2-氯苯基)-2-(2,4-二氟苯基)氧
Figure TW201945344A_D0081
-2-基]甲基}-2,4-二氫-3H-1,2,4-三唑-3-硫酮、(1.058)2-{[rel(2R,3S)-3-(2-氯苯基)-2-(2,4-二氟苯基)氧
Figure TW201945344A_D0082
-2-基]甲基}-2,4-二氫-3H-1,2,4-三唑-3-硫酮、(1.059)5-(4-氯苯甲基)-2-(氯甲基)-2-甲基-1-(1H-1,2,4-三唑-1-基甲基)環戊醇、(1.060)5-(烯丙基氫硫基)-1-{[3-(2-氯苯基)-2-(2,4-二氟苯基)氧
Figure TW201945344A_D0083
-2-基]甲基}-1H-1,2,4-三唑、(1.061)5-(烯丙基氫硫基)-1-{[rel(2R,3R)-3-(2-氯苯基)-2-(2,4-二氟苯基)氧
Figure TW201945344A_D0084
-2-基]甲基}-1H-1,2,4-三唑、(1.062)5-(烯丙基氫硫基)-1-{[rel(2R,3S)-3-(2-氯苯基)-2-(2,4-二氟苯基)氧
Figure TW201945344A_D0085
-2-基]甲基}-1H-1,2,4-三唑、(1.063)N'-(2,5-二甲基-4-{[3-(1,1,2,2-四氟乙氧基)苯基]氫硫基}苯基)-N-乙基-N-甲基亞胺甲醯胺、(1.064)N'-(2,5-二甲基-4-{[3-(2,2,2-三氟乙氧基)苯基]氫硫基}苯基)-N-乙基-N-甲基亞胺甲醯胺、(1.065)N'-(2,5-二甲基-4-{[3-(2,2,3,3-四氟丙氧基)苯基]氫硫基}苯基)-N-乙基-N-甲基亞胺甲醯胺、(1.066)N'-(2,5-二甲基-4-{[3-(五氟乙氧基)苯基]氫硫基}苯基)-N-乙基-N-甲基亞胺甲醯胺、(1.067)N'-(2,5-二甲基-4-{3-[(1,1,2,2-四氟乙基)氫硫基]苯氧基}苯基)-N-乙基-N-甲基亞胺甲醯胺、(1.068)N'-(2,5-二甲基-4-{3-[(2,2,2-三氟乙基)氫硫基]苯氧基}苯基)-N-乙基-N-甲基亞胺甲醯胺、(1.069)N'-(2,5-二甲基-4-{3-[(2,2,3,3-四氟丙基)氫硫基]苯氧基}苯基)-N-乙基-N-甲基亞胺甲醯胺、(1.070)N'-(2,5-二甲基-4-{3-[(五氟乙基)氫硫基]苯氧基}苯基)-N-乙基-N-甲基亞胺甲醯胺、(1.071)N'-(2,5-二甲基-4-苯氧基苯基)-N-乙基-N-甲基亞胺甲醯胺、(1.072)N'-(4-{[3-(二氟甲氧基)苯基]氫硫基}-2,5-二甲基苯基)-N-乙基-N-甲基亞胺甲醯胺、(1.073)N'-(4-{3-[(二氟甲基)氫硫基]苯氧基}-2,5-二甲基苯基)-N-乙基-N-甲基亞胺甲醯胺、(1.074)N'-[5-溴-6-(2,3-二氫-1H-茚-2-基氧基)-2-甲基吡啶-3-基]-N-乙基-N-甲基亞胺甲醯胺、(1.075)N'-{4-[(4,5-二氯-1,3-噻唑-2-基)氧基]-2,5-二甲基苯基}-N-乙基-N-甲基亞胺甲醯胺、(1.076)N'-{5-溴-6-[(1R)-1-(3,5-二氟苯基)乙氧基]-2-甲基吡啶-3-基}-N-乙基-N-甲基亞胺甲醯胺、(1.077)N'-{5-溴-6-[(1S)-1-(3,5-二氟苯基)乙氧基]-2-甲基吡啶-3-基}-N-乙基-N-甲基亞胺甲醯胺、(1.078)N'-{5-溴-6-[(順式-4-異丙基環己基)氧基]-2-甲基吡啶 -3-基}-N-乙基-N-甲基亞胺甲醯胺、(1.079)N'-{5-溴-6-[(反式-4-異丙基環己基)氧基]-2-甲基吡啶-3-基}-N-乙基-N-甲基亞胺甲醯胺、(1.080)N'-{5-溴-6-[1-(3,5-二氟苯基)乙氧基]-2-甲基吡啶-3-基}-N-乙基-N-甲基亞胺甲醯胺、(1.081)氯氟醚菌唑(Mefentrifluconazole)、(1.082)Ipfentrifluconazole、(1.083)2-[6-(4-溴苯氧基)-2-(三氟甲基)-3-吡啶基]-1-(1,2,4-三唑-1-基)丙-2-醇。 1) Inhibitors of ergosterol biosynthesis, such as (1.001) Cyproconazole, (1.002) Difenoconazole, (1.003) Epoxiconazole, (1.004) fenhexamid ), (1.005) fenpropidin, (1.006) fenpropimorph, (1.007) fenpyrazamine, (1.008) fluquinconazole, (1.009) hufenfen (flutriafol), (1.010) imazalil, (1.011) imazalil sulfate, (1.012) ipconazole, (1.013) metconazole, (1.014) Mike Myclobutanil, (1.015) paclobutrazol, (1.016) prochloraz, (1.017) propiconazole, (1.018) prothioconazole, (1.019)
Figure TW201945344A_D0073
Pyrisoxazole, (1.020) spiroxamine, (1.021) tebuconazole, (1.022) tetraconazole, (1.023) triadimenol, (1.024) tridemorpholine (tridemorph), (1.025) triticonazole, (1.026) (1R, 2S, 5S) -5- (4-chlorobenzyl) -2- (chloromethyl) -2-methyl-1- (1H-1,2,4-triazol-1-ylmethyl) cyclopentanol, (1.027) (1S, 2R, 5R) -5- (4-chlorobenzyl) -2- (chloromethyl ) -2-methyl-1- (1H-1,2,4-triazol-1-ylmethyl) cyclopentanol, (1.028) (2R) -2- (1-chlorocyclopropyl) -4 -[(1R) -2,2-dichlorocyclopropyl] -1- (1H-1,2,4-triazol-1-yl) but-2-ol, (1.029) (2R) -2- (1-chlorocyclopropyl) -4-[(1S) -2,2-dichlorocyclopropyl] -1- (1H-1,2,4-triazol-1-yl) but-2-ol (1.030) (2R) -2- [4- (4-chlorophenoxy) -2- (trifluoromethyl) phenyl] -1- (1H-1,2,4-triazole-1- Propyl) propan-2-ol, (1.031) (2S) -2- (1-chlorocyclopropyl) -4-[(1R) -2,2-dichlorocyclopropyl] -1- (1H-1 , 2,4-triazol-1-yl) but-2-ol, (1.032) (2S) -2- (1-chlorocyclopropyl) -4-[(1S) -2,2-dichlorocyclo Propyl] -1- (1H-1,2,4-triazol-1-yl) but-2-ol, (1.033) (2S) -2- [4- (4-chlorophenoxy) -2 -(Trifluoromethyl) phenyl] -1- (1H-1,2,4-triazol-1-yl) propan-2- Alcohol, (1.034) (R)-[3- (4-chloro-2-fluorophenyl) -5- (2,4-difluorophenyl) -1,2-
Figure TW201945344A_D0074
Azole-4-yl] (pyridin-3-yl) methanol, (1.035) (S)-[3- (4-chloro-2-fluorophenyl) -5- (2,4-difluorophenyl)- 1,2-
Figure TW201945344A_D0075
Azole-4-yl] (pyridin-3-yl) methanol, (1.036) [3- (4-chloro-2-fluorophenyl) -5- (2,4-difluorophenyl) -1,2-
Figure TW201945344A_D0076
Azole-4-yl] (pyridin-3-yl) methanol, (1.037) 1-({(2R, 4S) -2- [2-chloro-4- (4-chlorophenoxy) phenyl] -4 -Methyl-1,3-dioxolane-2-yl} methyl) -1H-1,2,4-triazole, (1.038) 1-(((2S, 4S) -2- [2- Chloro-4- (4-chlorophenoxy) phenyl] -4-methyl-1,3-dioxolane-2-yl} methyl) -1H-1,2,4-triazole, ( 1.039) 1-{[3- (2-chlorophenyl) -2- (2,4-difluorophenyl) oxy
Figure TW201945344A_D0077
-2-yl] methyl} -1H-1,2,4-triazol-5-ylthiocyanate, (1.040) 1-{[rel (2R, 3R) -3- (2-chlorophenyl ) -2- (2,4-difluorophenyl) oxy
Figure TW201945344A_D0078
-2-yl] methyl} -1H-1,2,4-triazol-5-ylthiocyanate, (1.041) 1-{[rel (2R, 3S) -3- (2-chlorophenyl ) -2- (2,4-difluorophenyl) oxy
Figure TW201945344A_D0079
-2-yl] methyl} -1H-1,2,4-triazol-5-ylthiocyanate, (1.042) 2-[(2R, 4R, 5R) -1- (2,4-di (Chlorophenyl) -5-hydroxy-2,6,6-trimethylhept-4-yl] -2,4-dihydro-3H-1,2,4-triazole-3-thione, (1.043 ) 2-[(2R, 4R, 5S) -1- (2,4-dichlorophenyl) -5-hydroxy-2,6,6-trimethylhept-4-yl] -2,4-di Hydrogen-3H-1,2,4-triazole-3-thione, (1.044) 2-[(2R, 4S, 5R) -1- (2,4-dichlorophenyl) -5-hydroxy-2 , 6,6-trimethylhept-4-yl] -2,4-dihydro-3H-1,2,4-triazol-3-thione, (1.045) 2-[(2R, 4S, 5S ) -1- (2,4-dichlorophenyl) -5-hydroxy-2,6,6-trimethylhept-4-yl] -2,4-dihydro-3H-1,2,4- Triazole-3-thione, (1.046) 2-[(2S, 4R, 5R) -1- (2,4-dichlorophenyl) -5-hydroxy-2,6,6-trimethylheptane- 4-yl] -2,4-dihydro-3H-1,2,4-triazole-3-thione, (1.047) 2-[(2S, 4R, 5S) -1- (2,4-di (Chlorophenyl) -5-hydroxy-2,6,6-trimethylhept-4-yl] -2,4-dihydro-3H-1,2,4-triazole-3-thione, (1.048 ) 2-[(2S, 4S, 5R) -1- (2,4-dichlorophenyl) -5-hydroxy-2,6,6-trimethylhept-4-yl] -2,4-di Hydrogen-3H-1,2,4-triazole-3-thione, (1.049) 2-[(2S, 4S, 5S) -1- (2,4-dichlorophenyl) -5-hydroxy-2 , 6,6-trimethylhept-4-yl] -2,4-dihydro-3H-1,2,4-triazole-3-thione, (1.050) 2- [1- (2,4 -Dichlorophenyl ) -5-hydroxy-2,6,6-trimethylhept-4-yl] -2,4-dihydro-3H-1,2,4-triazole-3-thione, (1.051) 2- [2-Chloro-4- (2,4-dichlorophenoxy) phenyl] -1- (1H-1,2,4-triazol-1-yl) propan-2-ol, (1.052) 2 -[2-chloro-4- (4-chlorophenoxy) phenyl] -1- (1H-1,2,4-triazol-1-yl) but-2-ol, (1.053) 2- [ 4- (4-chlorophenoxy) -2- (trifluoromethyl) phenyl] -1- (1H-1,2,4-triazol-1-yl) but-2-ol, (1.054) 2- [4- (4-chlorophenoxy) -2- (trifluoromethyl) phenyl] -1- (1H-1,2,4-triazol-1-yl) pent-2-ol, (1.055) 2- [4- (4-chlorophenoxy) -2- (trifluoromethyl) phenyl] -1- (1H-1,2,4-triazol-1-yl) propan-2 -Alcohol, (1.056) 2-{[3- (2-chlorophenyl) -2- (2,4-difluorophenyl) oxy
Figure TW201945344A_D0080
-2-yl] methyl} -2,4-dihydro-3H-1,2,4-triazole-3-thione, (1.057) 2-{[rel (2R, 3R) -3- (2 -Chlorophenyl) -2- (2,4-difluorophenyl) oxy
Figure TW201945344A_D0081
-2-yl] methyl} -2,4-dihydro-3H-1,2,4-triazole-3-thione, (1.058) 2-{[rel (2R, 3S) -3- (2 -Chlorophenyl) -2- (2,4-difluorophenyl) oxy
Figure TW201945344A_D0082
-2-yl] methyl} -2,4-dihydro-3H-1,2,4-triazole-3-thione, (1.059) 5- (4-chlorobenzyl) -2- (chloro (Methyl) -2-methyl-1- (1H-1,2,4-triazol-1-ylmethyl) cyclopentanol, (1.060) 5- (allylhydrothio) -1- { (3- (2-chlorophenyl) -2- (2,4-difluorophenyl) oxy
Figure TW201945344A_D0083
2-yl] methyl} -1H-1,2,4-triazole, (1.061) 5- (allylhydrothio) -1-{[rel (2R, 3R) -3- (2- (Chlorophenyl) -2- (2,4-difluorophenyl) oxy
Figure TW201945344A_D0084
2-yl] methyl} -1H-1,2,4-triazole, (1.062) 5- (allylhydrothio) -1-{[rel (2R, 3S) -3- (2- (Chlorophenyl) -2- (2,4-difluorophenyl) oxy
Figure TW201945344A_D0085
-2-yl] methyl} -1H-1,2,4-triazole, (1.063) N '-(2,5-dimethyl-4-{[3- (1,1,2,2- Tetrafluoroethoxy) phenyl] hydrothio} phenyl) -N-ethyl-N-methylimine formamide, (1.064) N '-(2,5-dimethyl-4- { (3- (2,2,2-trifluoroethoxy) phenyl] hydrothio} phenyl) -N-ethyl-N-methylimine formamide, (1.065) N '-(2 , 5-dimethyl-4-{[3- (2,2,3,3-tetrafluoropropoxy) phenyl] hydrothio} phenyl) -N-ethyl-N-methylimine Formamidine, (1.066) N '-(2,5-dimethyl-4-{[3- (pentafluoroethoxy) phenyl] hydrothio} phenyl) -N-ethyl-N- Methylimine formamidine, (1.067) N '-(2,5-dimethyl-4- {3-[(1,1,2,2-tetrafluoroethyl) hydrosulfanyl] phenoxy } Phenyl) -N-ethyl-N-methylimine formamide, (1.068) N '-(2,5-dimethyl-4- {3-[(2,2,2-trifluoro Ethyl) hydrothio] phenoxy} phenyl) -N-ethyl-N-methylimine formamide, (1.069) N '-(2,5-dimethyl-4- {3- [(2,2,3,3-tetrafluoropropyl) hydrothio] phenoxy} phenyl) -N-ethyl-N-methylimine formamide, (1.070) N '-(2 , 5-dimethyl-4- {3-[(pentafluoroethyl) hydrothio] phenoxy} phenyl) -N-ethyl-N-methylimine formamide, (1.071) N '-(2,5-dimethyl-4-phenoxyphenyl) -N-ethyl-N-form Imine formamide, (1.072) N '-(4-{[3- (difluoromethoxy) phenyl] hydrothio} -2,5-dimethylphenyl) -N-ethyl- N-methylimine formamidine, (1.073) N '-(4- {3-[(difluoromethyl) hydrosulfanyl] phenoxy} -2,5-dimethylphenyl) -N -Ethyl-N-methylimine formamide, (1.074) N '-[5-bromo-6- (2,3-dihydro-1H-inden-2-yloxy) -2-methyl Pyridine-3-yl] -N-ethyl-N-methylimine formamide, (1.075) N '-{4-[(4,5-dichloro-1,3-thiazol-2-yl) Oxy] -2,5-dimethylphenyl} -N-ethyl-N-methylimine formamide, (1.076) N '-{5-bromo-6-[(1R) -1- (3,5-difluorophenyl) ethoxy] -2-methylpyridin-3-yl} -N-ethyl-N-methylimine formamide, (1.077) N '-{5- Bromo-6-[(1S) -1- (3,5-difluorophenyl) ethoxy] -2-methylpyridin-3-yl} -N-ethyl-N-methylimide Amine, (1.078) N '-{5-bromo-6-[(cis-4-isopropylcyclohexyl) oxy] -2-methylpyridin-3-yl} -N-ethyl-N- Methylimine formamidine, (1.079) N '-{5-bromo-6-[(trans-4-isopropylcyclohexyl) oxy] -2-methylpyridin-3-yl} -N -Ethyl-N-methylimine formamide, (1.080) N '-{5-bromo-6- [1- (3,5-difluorophenyl) ethoxy] -2-methylpyridine -3-yl} -N-ethyl-N-methylidene Formamidine, (1.081) Mefentrifluconazole, (1.082) Ipfentrifluconazole, (1.083) 2- [6- (4-bromophenoxy) -2- (trifluoromethyl) -3-pyridine Group] -1- (1,2,4-triazol-1-yl) propan-2-ol.

2)呼吸鏈複合物I或II之抑制劑，例如(2.001)苯并烯氟菌唑(benzovindiflupyr)、(2.002)聯苯吡菌胺(bixafen)、(2.003)白克列(boscalid)、(2.004)萎銹靈(carboxin)、(2.005)氟派瑞(fluopyram)、(2.006)福多寧(flutolanil)、(2.007)氟克殺(fluxapyroxad)、(2.008)福拉比(furametpyr)、(2.009)異丙噻菌胺(isofetamid)、(2.010)亞派占(isopyrazam)(逆-表異構鏡像異構物1R,4S,9S)、(2.011)亞派占(逆-表異構鏡像異構物1S,4R,9R)、(2.012)亞派占(逆-表異構外消旋物1RS,4SR,9SR)、(2.013)亞派占(同-表異構外消旋物1RS,4SR,9RS與逆-表異構外消旋物1RS,4SR,9SR之混合物)、(2.014)亞派占(同-表異構鏡像異構物1R,4S,9R)、(2.015)亞派占(順式差向異構對映體1S,4R,9S)、(2.016)亞派占(同-表異構外消旋物1RS,4SR,9RS)、(2.017)戊苯吡菌胺(penflufen)、(2.018)吡噻菌胺(penthiopyrad)、(2.019)氟唑菌醯羥胺(pydiflumetofen)、(2.020)pyraziflumid、(2.021)氟唑環菌胺(sedaxane)、(2.022)1,3-二甲基-N-(1,1,3-三甲基-2,3-二氫-1H-茚-4-基)-1H-吡唑-4-甲醯胺、(2.023)1,3-二甲基-N-[(3R)-1,1,3-三甲基-2,3-二氫-1H-茚-4-基]-1H-吡唑-4-甲醯胺、(2.024)1,3-二甲基-N-[(3S)-1,1,3-三甲基-2,3-二氫-1H-茚-4-基]-1H-吡唑-4-甲醯胺、(2.025)1-甲基-3-(三氟甲基)-N-[2'-(三氟甲基)聯苯-2-基]-1H-吡唑-4-甲醯胺、(2.026)2-氟-6-(三氟甲基)-N-(1,1,3-三甲基-2,3-二氫-1H-茚-4-基)苯甲醯胺、(2.027)3-(二氟甲基)-1-甲基-N-(1,1,3-三甲基-2,3-二氫-1H-茚-4-基)-1H-吡唑-4-甲醯胺(俗名：inpyrfluxam)、(2.028)3-(二氟甲基)-1-甲基-N-[(3R)-1,1,3-三甲基-2,3-二氫-1H-茚-4-基]-1H-吡唑-4-甲醯胺、(2.029)3-(二氟甲基)-1-甲基-N-[(3S)-1,1,3-三甲基-2,3-二氫-1H-茚-4-基]-1H-吡唑-4-甲醯胺、(2.030)3-(二氟甲基)-N-(7-氟-1,1,3-三甲基-2,3-二氫-1H-茚-4-基)-1-甲基-1H-吡唑-4-甲醯胺(俗名：fluindapyr)、(2.031)3-(二氟甲基)-N-[(3R)-7-氟-1,1,3-三甲基 -2,3-二氫-1H-茚-4-基]-1-甲基-1H-吡唑-4-甲醯胺、(2.032)3-(二氟甲基)-N-[(3S)-7-氟-1,1,3-三甲基-2,3-二氫-1H-茚-4-基]-1-甲基-1H-吡唑-4-甲醯胺、(2.033)5,8-二氟-N-[2-(2-氟-4-{[4-(三氟甲基)吡啶-2-基]氧基}苯基)乙基]喹唑啉-4-胺、(2.034)N-(2-環戊基-5-氟苯甲基)-N-環丙基-3-(二氟甲基)-5-氟-1-甲基-1H-吡唑-4-甲醯胺、(2.035)N-(2-第三丁基-5-甲基苯甲基)-N-環丙基-3-(二氟甲基)-5-氟-1-甲基-1H-吡唑-4-甲醯胺、(2.036)N-(2-第三丁基苯甲基)-N-環丙基-3-(二氟甲基)-5-氟-1-甲基-1H-吡唑-4-甲醯胺、(2.037)N-(5-氯-2-乙基苯甲基)-N-環丙基-3-(二氟甲基)-5-氟-1-甲基-1H-吡唑-4-甲醯胺、(2.038)N-(5-氯-2-異丙基苯甲基)-N-環丙基-3-(二氟甲基)-5-氟-1-甲基-1H-吡唑-4-甲醯胺、(2.039)N-[(1R,4S)-9-(二氯伸甲基)-1,2,3,4-四氫-1,4-亞甲基萘-5-基]-3-(二氟甲基)-1-甲基-1H-吡唑-4-甲醯胺、(2.040)N-[(1S,4R)-9-(二氯伸甲基)-1,2,3,4-四氫-1,4-亞甲基萘-5-基]-3-(二氟甲基)-1-甲基-1H-吡唑-4-甲醯胺、(2.041)N-[1-(2,4-二氯苯基)-1-甲氧基丙-2-基]-3-(二氟甲基)-1-甲基-1H-吡唑-4-甲醯胺、(2.042)N-[2-氯-6-(三氟甲基)苯甲基]-N-環丙基-3-(二氟甲基)-5-氟-1-甲基-1H-吡唑-4-甲醯胺、(2.043)N-[3-氯-2-氟-6-(三氟甲基)苯甲基]-N-環丙基-3-(二氟甲基)-5-氟-1-甲基-1H-吡唑-4-甲醯胺、(2.044)N-[5-氯-2-(三氟甲基)苯甲基]-N-環丙基-3-(二氟甲基)-5-氟-1-甲基-1H-吡唑-4-甲醯胺、(2.045)N-環丙基-3-(二氟甲基)-5-氟-1-甲基-N-[5-甲基-2-(三氟甲基)苯甲基]-1H-吡唑-4-甲醯胺、(2.046)N-環丙基-3-(二氟甲基)-5-氟-N-(2-氟-6-異丙基苯甲基)-1-甲基-1H-吡唑-4-甲醯胺、(2.047)N-環丙基-3-(二氟甲基)-5-氟-N-(2-異丙基-5-甲基苯甲基)-1-甲基-1H-吡唑-4-甲醯胺、(2.048)N-環丙基-3-(二氟甲基)-5-氟-N-(2-異丙基苯甲基)-1-甲基-1H-吡唑-4-硫代醯胺、(2.049)N-環丙基-3-(二氟甲基)-5-氟-N-(2-異丙基苯甲基)-1-甲基-1H-吡唑-4-甲醯胺、(2.050)N-環丙基-3-(二氟甲基)-5-氟-N-(5-氟-2-異丙基苯甲基)-1-甲基-1H-吡唑-4-甲醯胺、(2.051)N-環丙基-3-(二氟甲基)-N-(2-乙基-4,5-二甲基苯甲基)-5-氟-1-甲基-1H-吡唑-4-甲醯胺、(2.052)N-環丙基-3-(二氟甲基)-N-(2-乙基-5-氟苯甲基)-5-氟-1-甲基-1H-吡唑-4-甲醯胺、(2.053)N-環丙基-3-(二氟甲基)-N-(2-乙基-5-甲基苯甲基)-5-氟-1-甲基-1H-吡 唑-4-甲醯胺、(2.054)N-環丙基-N-(2-環丙基-5-氟苯甲基)-3-(二氟甲基)-5-氟-1-甲基-1H-吡唑-4-甲醯胺、(2.055)N-環丙基-N-(2-環丙基-5-甲基苯甲基)-3-(二氟甲基)-5-氟-1-甲基-1H-吡唑-4-甲醯胺、(2.056)N-環丙基-N-(2-環丙基苯甲基)-3-(二氟甲基)-5-氟-1-甲基-1H-吡唑-4-甲醯胺。 2) Inhibitors of respiratory chain complexes I or II, such as (2.001) benzovindiflupyr, (2.002) bixafen, (2.003) boscalid, ( 2.004) carboxin, (2.005) fluopyram, (2.006) flutolanil, (2.007) fluxapyroxad, (2.008) furametpyr, (2.008) 2.009) isofetamid, (2.010) isopyrazam (reverse-epimeric mirror isomers 1R, 4S, 9S), (2.011) apyrezami (reverse-epimeric mirror Isomers 1S, 4R, 9R), (2.012) Subazhan (reverse-epimeric racemate 1RS, 4SR, 9SR), (2.013) Subazhan (iso-epimeric racemate 1RS) , 4SR, 9RS and the mixture of the reverse-epimeric racemate 1RS, 4SR, 9SR), (2.014) Subazhan (iso-epimeric mirror isomers 1R, 4S, 9R), (2.015) Pyrazine (cis-episomeric enantiomers 1S, 4R, 9S), (2.016) Sub-pyrazine (iso-epi-racemic racemates 1RS, 4SR, 9RS), (2.017) Penfenpyram (penflufen), (2.018) penthiopyrad, (2.019) fluazolidine (pydiflumetofen), (2.020) pyraziflumid, (2.021) fluoxazol (sedaxane), (2.022) 1,3 -Second -N- (1,1,3-trimethyl-2,3-dihydro-1H-inden-4-yl) -1H-pyrazole-4-carboxamide, (2.023) 1,3-dimethyl -N-[(3R) -1,1,3-trimethyl-2,3-dihydro-1H-inden-4-yl] -1H-pyrazole-4-carboxamide, (2.024) 1 , 3-dimethyl-N-[(3S) -1,1,3-trimethyl-2,3-dihydro-1H-inden-4-yl] -1H-pyrazole-4-carboxamide (2.025) 1-methyl-3- (trifluoromethyl) -N- [2 '-(trifluoromethyl) biphenyl-2-yl] -1H-pyrazole-4-carboxamide, ( 2.026) 2-fluoro-6- (trifluoromethyl) -N- (1,1,3-trimethyl-2,3-dihydro-1H-inden-4-yl) benzamide, (2.027 ) 3- (difluoromethyl) -1-methyl-N- (1,1,3-trimethyl-2,3-dihydro-1H-inden-4-yl) -1H-pyrazole-4 -Formamidine (common name: inpyrfluxam), (2.028) 3- (difluoromethyl) -1-methyl-N-[(3R) -1,1,3-trimethyl-2,3-dihydro -1H-inden-4-yl] -1H-pyrazole-4-carboxamide, (2.029) 3- (difluoromethyl) -1-methyl-N-[(3S) -1,1,3 -Trimethyl-2,3-dihydro-1H-inden-4-yl] -1H-pyrazole-4-carboxamide, (2.030) 3- (difluoromethyl) -N- (7-fluoro -1,1,3-trimethyl-2,3-dihydro-1H-inden-4-yl) -1-methyl-1H-pyrazole-4-carboxamide (common name: fluindapyr), (2.031 ) 3- (difluoromethyl) -N-[(3R) -7-fluoro-1,1,3-trimethyl-2,3-dihydro-1H-inden-4-yl] -1-methyl Yl-1H-pyrazole-4 -Formamidine, (2.032) 3- (difluoromethyl) -N-[(3S) -7-fluoro-1,1,3-trimethyl-2,3-dihydro-1H-indene-4 -Yl] -1-methyl-1H-pyrazole-4-carboxamide, (2.033) 5,8-difluoro-N- [2- (2-fluoro-4-{[4- (trifluoromethyl Yl) pyridin-2-yl] oxy} phenyl) ethyl] quinazolin-4-amine, (2.034) N- (2-cyclopentyl-5-fluorobenzyl) -N-cyclopropyl -3- (difluoromethyl) -5-fluoro-1-methyl-1H-pyrazole-4-carboxamide, (2.035) N- (2-tert-butyl-5-methylbenzyl ) -N-cyclopropyl-3- (difluoromethyl) -5-fluoro-1-methyl-1H-pyrazole-4-carboxamide, (2.036) N- (2-third butylbenzene (Methyl) -N-cyclopropyl-3- (difluoromethyl) -5-fluoro-1-methyl-1H-pyrazole-4-carboxamide, (2.037) N- (5-chloro-2 -Ethylbenzyl) -N-cyclopropyl-3- (difluoromethyl) -5-fluoro-1-methyl-1H-pyrazole-4-carboxamide, (2.038) N- (5 -Chloro-2-isopropylbenzyl) -N-cyclopropyl-3- (difluoromethyl) -5-fluoro-1-methyl-1H-pyrazole-4-carboxamide, (2.039 ) N-[(1R, 4S) -9- (Dichloromethylene) -1,2,3,4-tetrahydro-1,4-methylenenaphthalene-5-yl] -3- (difluoro (Methyl) -1-methyl-1H-pyrazole-4-carboxamide, (2.040) N-[(1S, 4R) -9- (dichloromethyl) -1,2,3,4- Tetrahydro-1,4-methylenenaphthalene-5-yl] -3- (difluoromethyl) -1-methyl-1H-pyrazole-4- Amidine, (2.041) N- [1- (2,4-dichlorophenyl) -1-methoxyprop-2-yl] -3- (difluoromethyl) -1-methyl-1H- Pyrazole-4-carboxamide, (2.042) N- [2-chloro-6- (trifluoromethyl) benzyl] -N-cyclopropyl-3- (difluoromethyl) -5-fluoro 1-methyl-1H-pyrazole-4-carboxamide, (2.043) N- [3-chloro-2-fluoro-6- (trifluoromethyl) benzyl] -N-cyclopropyl- 3- (difluoromethyl) -5-fluoro-1-methyl-1H-pyrazole-4-carboxamide, (2.044) N- [5-chloro-2- (trifluoromethyl) benzyl ] -N-cyclopropyl-3- (difluoromethyl) -5-fluoro-1-methyl-1H-pyrazole-4-carboxamide, (2.045) N-cyclopropyl-3- (di (Fluoromethyl) -5-fluoro-1-methyl-N- [5-methyl-2- (trifluoromethyl) benzyl] -1H-pyrazole-4-carboxamide, (2.046) N -Cyclopropyl-3- (difluoromethyl) -5-fluoro-N- (2-fluoro-6-isopropylbenzyl) -1-methyl-1H-pyrazole-4-carboxamide (2.047) N-cyclopropyl-3- (difluoromethyl) -5-fluoro-N- (2-isopropyl-5-methylbenzyl) -1-methyl-1H-pyrazole 4-formamidine, (2.048) N-cyclopropyl-3- (difluoromethyl) -5-fluoro-N- (2-isopropylbenzyl) -1-methyl-1H-pyridine Azole-4-thiofluorenamine, (2.049) N-cyclopropyl-3- (difluoromethyl) -5-fluoro-N- (2-isopropylbenzyl) -1-methyl-1H -Pyrazole-4-carboxamide, (2.050) N-cyclopropane Methyl-3- (difluoromethyl) -5-fluoro-N- (5-fluoro-2-isopropylbenzyl) -1-methyl-1H-pyrazole-4-carboxamide, (2.051 ) N-cyclopropyl-3- (difluoromethyl) -N- (2-ethyl-4,5-dimethylbenzyl) -5-fluoro-1-methyl-1H-pyrazole- 4-formamidine, (2.052) N-cyclopropyl-3- (difluoromethyl) -N- (2-ethyl-5-fluorobenzyl) -5-fluoro-1-methyl-1H -Pyrazole-4-carboxamide, (2.053) N-cyclopropyl-3- (difluoromethyl) -N- (2-ethyl-5-methylbenzyl) -5-fluoro-1 -Methyl-1H-pyrazole-4-carboxamide, (2.054) N-cyclopropyl-N- (2-cyclopropyl-5-fluorobenzyl) -3- (difluoromethyl)- 5-fluoro-1-methyl-1H-pyrazole-4-carboxamide, (2.055) N-cyclopropyl-N- (2-cyclopropyl-5-methylbenzyl) -3- ( Difluoromethyl) -5-fluoro-1-methyl-1H-pyrazole-4-carboxamide, (2.056) N-cyclopropyl-N- (2-cyclopropylbenzyl) -3- (Difluoromethyl) -5-fluoro-1-methyl-1H-pyrazole-4-carboxamide.

3)呼吸鏈複合物III之抑制劑，例如(3.001)滅脫定(ametoctradin)、(3.002)安美速(amisulbrom)、(3.003)亞托敏(azoxystrobin)、(3.004)甲香菌酯(coumethoxystrobin)、(3.005)丁香菌酯(coumoxystrobin)、(3.006)賽座滅(cyazofamid)、(3.007)醚菌胺(dimoxystrobin)、(3.008)烯肟菌酯(enoxastrobin)、(3.009)凡殺同(famoxadon)、(3.010)咪唑菌酮(fenamidon)、(3.011)氟菌蟎酯(flufenoxystrobin)、(3.012)氟嘧菌酯(fluoxastrobin)、(3.013)克收欣(kresoxim-methyl)、(3.014)苯氧菌胺(metominostrobin)、(3.015)肟醚菌胺(orysastrobin)、(3.016)啶氧菌酯(picoxystrobin)、(3.017)百克敏(pyraclostrobin)、(3.018)唑胺菌酯(pyrametostrobin)、(3.019)唑菌酯(pyraoxystrobin)、(3.020)三氟敏(trifloxystrobin)、(3.021)(2E)-2-{2-[({[(1E)-1-(3-{[(E)-1-氟-2-苯基乙烯基]氧基}苯基)亞乙基]胺基}氧基)甲基]苯基}-2-(甲氧基亞胺基)-N-甲基乙醯胺、(3.022)(2E,3Z)-5-{[1-(4-氯苯基)-1H-吡唑--3-基]氧基}-2-(甲氧基亞胺基)-N,3-二甲基戊-3-烯醯胺、(3.023)(2R)-2-{2-[(2,5-二甲基苯氧基)甲基]苯基}-2-甲氧基-N-甲基乙醯胺、(3.024)(2S)-2-{2-[(2,5-二甲基苯氧基)甲基]苯基}-2-甲氧基-N-甲基乙醯胺、(3.025)(3S,6S,7R,8R)-8-苯甲基-3-[({3-[(異丁醯基氧基)甲氧基]-4-甲氧基吡啶-2-基}羰基)胺基]-6-甲基-4,9-二側氧-1,5-二氧戊環-7-基2-甲基丙酸酯(俗名：fenpicoxamid)、(3.026)2-{2-[(2,5-二甲基-苯氧基)甲基]苯基}-2-甲氧基-N-甲基乙醯胺、(3.027)N-(3-乙基-3,5,5-三甲基環己基)-3-甲醯胺基-2-羥基苯甲醯胺、(3.028)(2E,3Z)-5-{[1-(4-氯-2-氟苯基)-1H-吡唑-3-基]氧基}-2-(甲氧基亞胺基)-N,3-二甲基戊-3-烯醯胺、(3.029)甲基{5-[3-(2,4-二甲基苯基)-1H-吡唑-1-基]-2-甲基苯甲基}胺甲酸酯、(3.030)(1S)-2,2-雙(4-氟苯基)-1-甲基乙基N-{[3-(乙醯基氧基)-4-甲氧基-2-吡啶基]羰基}-L-丙胺酸酯、(3.031)florylpicoxamid。 3) Inhibitors of respiratory chain complex III, such as (3.001) ametoctradin, (3.002) amisulbrom, (3.003) azoxystrobin, (3.004) coumethoxystrobin ), (3.005) coumoxystrobin, (3.006) cyazofamid, (3.007) dimoxystrobin, (3.008) enoxastrobin, (3.009) famoxadon), (3.010) fenamidon, (3.011) flufenoxystrobin, (3.012) fluoxastrobin, (3.013) kresoxim-methyl, (3.014) Metominostrobin, (3.015) orysastrobin, (3.016) picoxystrobin, (3.017) pyraclostrobin, (3.018) pyrametostrobin, (3.019) pyraoxystrobin, (3.020) trifloxystrobin, (3.021) (2E) -2- {2-[(((((1E) -1- (3-(((E) -1-fluoro-2-phenylvinyl] oxy} phenyl) ethylidene] amino} oxy) methyl] phenyl} -2- (methoxyimino) -N-methyl Acetylamine, (3.022) (2E, 3Z) -5-{[1- (4-chlorophenyl) -1H-pyrazole--3-yl] oxy} -2- (methoxyimino ) -N, 3- Methylpent-3-enamidamine, (3.023) (2R) -2- {2-[(2,5-dimethylphenoxy) methyl] phenyl} -2-methoxy-N- Methylacetamide, (3.024) (2S) -2- {2-[(2,5-dimethylphenoxy) methyl] phenyl} -2-methoxy-N-methylacetamidine Amine, (3.025) (3S, 6S, 7R, 8R) -8-benzyl-3-[({3-[(isobutylfluorenyloxy) methoxy] -4-methoxypyridin-2-yl } Carbonyl) amino] -6-methyl-4,9-dioxo-1,5-dioxolane-7-yl 2-methylpropionate (common name: fenpicoxamid), (3.026) 2- {2-[(2,5-dimethyl-phenoxy) methyl] phenyl} -2-methoxy-N-methylacetamide, (3.027) N- (3-ethyl-3 , 5,5-trimethylcyclohexyl) -3-carboxamido-2-hydroxybenzamide, (3.028) (2E, 3Z) -5-{(1- (4-chloro-2-fluoro (Phenyl) -1H-pyrazol-3-yl] oxy} -2- (methoxyimino) -N, 3-dimethylpent-3-enamidamine, (3.029) methyl {5 -[3- (2,4-dimethylphenyl) -1H-pyrazol-1-yl] -2-methylbenzyl} carbamate, (3.030) (1 S ) -2,2 -Bis (4-fluorophenyl) -1-methylethylN-{[3- (ethylamidooxy) -4-methoxy-2-pyridyl] carbonyl} -L-alanine, (3.031) florylpicoxamid.

4)有絲分裂和細胞分裂之抑制劑，例如(4.001)貝芬替(carbendazim)、(4.002)乙黴威(diethofencarb)、(4.003)噻唑菌胺(ethaboxam)、(4.004)氟比來(fluopicolid)、(4.005)賓得克利(pencycuron)、(4.006)腐絕(thiabendazole)、(4.007)甲基多保淨(thiophanate-methyl)、(4.008)座賽胺(zoxamide)、(4.009)3-氯-4-(2,6-二氟苯基)-6-甲基-5-苯基嗒

Figure TW201945344A_D0086
、(4.010)3-氯-5-(4-氯苯基)-4-(2,6-二氟苯基)-6-甲基嗒
Figure TW201945344A_D0087
、(4.011)3-氯-5-(6-氯吡啶-3-基)-6-甲基-4-(2,4,6-三氟苯基)嗒
Figure TW201945344A_D0088
、(4.012)4-(2-溴-4-氟苯基)-N-(2,6-二氟苯基)-1,3-二甲基-1H-吡唑-5-胺、(4.013)4-(2-溴-4-氟苯基)-N-(2-溴-6-氟苯基)-1,3-二甲基-1H-吡唑-5-胺、(4.014)4-(2-溴-4-氟苯基)-N-(2-溴苯基)-1,3-二甲基-1H-吡唑-5-胺、(4.015)4-(2-溴-4-氟苯基)-N-(2-氯-6-氟苯基)-1,3-二甲基-1H-吡唑-5-胺、(4.016)4-(2-溴-4-氟苯基)-N-(2-氯苯基)-1,3-二甲基-1H-吡唑-5-胺、(4.017)4-(2-溴-4-氟苯基)-N-(2-氟苯基)-1,3-二甲基-1H-吡唑-5-胺、(4.018)4-(2-氯-4-氟苯基)-N-(2,6-二氟苯基)-1,3-二甲基-1H-吡唑-5-胺、(4.019)4-(2-氯-4-氟苯基)-N-(2-氯-6-氟苯基)-1,3-二甲基-1H-吡唑-5-胺、(4.020)4-(2-氯-4-氟苯基)-N-(2-氯苯基)-1,3-二甲基-1H-吡唑-5-胺、(4.021)4-(2-氯-4-氟苯基)-N-(2-氟苯基)-1,3-二甲基-1H-吡唑-5-胺、(4.022)4-(4-氯苯基)-5-(2,6-二氟苯基)-3,6-二甲基嗒
Figure TW201945344A_D0089
、(4.023)N-(2-溴-6-氟苯基)-4-(2-氯-4-氟苯基)-1,3-二甲基-1H-吡唑-5-胺、(4.024)N-(2-溴苯基)-4-(2-氯-4-氟苯基)-1,3-二甲基-1H-吡唑-5-胺、(4.025)N-(4-氯-2,6-二氟苯基)-4-(2-氯-4-氟苯基)-1,3-二甲基-1H-吡唑-5-胺。 4) Inhibitors of mitosis and cell division, such as (4.001) carbendazim, (4.002) diethofencarb, (4.003) ethaboxam, (4.004) fluopicolid , (4.005) pencycuron, (4.006) thiabendazole, (4.007) thiophanate-methyl, (4.008) zoxamide, (4.009) 3-chloro- 4- (2,6-difluorophenyl) -6-methyl-5-phenyl
Figure TW201945344A_D0086
(4.010) 3-chloro-5- (4-chlorophenyl) -4- (2,6-difluorophenyl) -6-methyl
Figure TW201945344A_D0087
(4.011) 3-chloro-5- (6-chloropyridin-3-yl) -6-methyl-4- (2,4,6-trifluorophenyl)
Figure TW201945344A_D0088
(4.012) 4- (2-bromo-4-fluorophenyl) -N- (2,6-difluorophenyl) -1,3-dimethyl-1H-pyrazole-5-amine, (4.013 ) 4- (2-bromo-4-fluorophenyl) -N- (2-bromo-6-fluorophenyl) -1,3-dimethyl-1H-pyrazole-5-amine, (4.014) 4 -(2-bromo-4-fluorophenyl) -N- (2-bromophenyl) -1,3-dimethyl-1H-pyrazole-5-amine, (4.015) 4- (2-bromo- 4-fluorophenyl) -N- (2-chloro-6-fluorophenyl) -1,3-dimethyl-1H-pyrazole-5-amine, (4.016) 4- (2-bromo-4- (Fluorophenyl) -N- (2-chlorophenyl) -1,3-dimethyl-1H-pyrazole-5-amine, (4.017) 4- (2-bromo-4-fluorophenyl) -N -(2-fluorophenyl) -1,3-dimethyl-1H-pyrazole-5-amine, (4.018) 4- (2-chloro-4-fluorophenyl) -N- (2,6- (Difluorophenyl) -1,3-dimethyl-1H-pyrazole-5-amine, (4.019) 4- (2-chloro-4-fluorophenyl) -N- (2-chloro-6-fluoro (Phenyl) -1,3-dimethyl-1H-pyrazole-5-amine, (4.020) 4- (2-chloro-4-fluorophenyl) -N- (2-chlorophenyl) -1, 3-dimethyl-1H-pyrazole-5-amine, (4.021) 4- (2-chloro-4-fluorophenyl) -N- (2-fluorophenyl) -1,3-dimethyl- 1H-pyrazole-5-amine, (4.022) 4- (4-chlorophenyl) -5- (2,6-difluorophenyl) -3,6-dimethyl
Figure TW201945344A_D0089
(4.023) N- (2-bromo-6-fluorophenyl) -4- (2-chloro-4-fluorophenyl) -1,3-dimethyl-1H-pyrazole-5-amine, ( 4.024) N- (2-bromophenyl) -4- (2-chloro-4-fluorophenyl) -1,3-dimethyl-1H-pyrazole-5-amine, (4.025) N- (4 -Chloro-2,6-difluorophenyl) -4- (2-chloro-4-fluorophenyl) -1,3-dimethyl-1H-pyrazole-5-amine.

5)具有多位點作用能力的化合物，例如(5.001)波爾多液(Bordeauxmixture)、(5.002)四氯丹(captafol)、(5.003)蓋普丹(captan)、(5.004)百菌清(chlorthalonil)、(5.005)氫氧化銅、(5.006)環烷酸銅、(5.007)氧化銅、(5.008)氯氧化銅、(5.009)硫酸銅(2+)、(5.010)二腈硫醌(dithianon)、(5.011)多果定(dodin)、(5.012)福爾培(folpet)、(5.013)鋅錳乃浦(mancozeb)、(5.014)代森錳(maneb)、(5.015)免得爛(metiram)、(5.016)免得爛鋅(metiram-zinc)、(5.017)快得寧(oxine copper)、(5.018)甲基鋅乃浦(propineb)、(5.019)包括石灰硫黃(calcium polysulfide)的硫和硫製備物、(5.020)得恩地(thiram)、(5.021)鋅 乃浦(zineb)、(5.022)吉闌(ziram)、(5.023)6-乙基-5,7-二側氧基-6,7-二氫-5H-吡咯并[3',4'：5,6][1,4]二硫雜環己烯并[2,3-c][1,2]噻唑-3-甲腈。 5) Compounds with multi-site action ability, such as (5.001) Bordeaux mixture, (5.002) captafol, (5.003) captan, (5.004) chlorthalonil , (5.005) copper hydroxide, (5.006) copper naphthenate, (5.007) copper oxide, (5.008) copper oxychloride, (5.009) copper sulfate (2+), (5.010) dithianon, (dithianon), (5.011) dodin, (5.012) folpet, (5.013) zinc manganese (mancozeb), (5.014) mancozeb (5.015) to avoid rotten (metiram), (5.016) Free from metiram-zinc, (5.017) oxine copper, (5.018) methyl zinc propineb, (5.019) sulfur and sulfur including calcium polysulfide Preparation, (5.020) thiram, (5.021) zineb, (5.022) ziram, (5.023) 6-ethyl-5,7-dioxo-6, 7-dihydro-5H-pyrrolo [3 ', 4': 5,6] [1,4] dithiacyclohexene [2,3-c] [1,2] thiazole-3-carbonitrile .

6)能引發宿主防禦的化合物，例如(6.001)阿拉酸式苯-S-甲基(acibenzolar-S-methyl)、(6.002)異噻菌胺(isotianil)、(6.003)撲殺熱(probenazole)、(6.004)噻醯菌胺(tiadinil)。 6) Compounds that can trigger host defenses, such as (6.001) acibenzolar-S-methyl, (6.002) isotianil, (6.003) probenazole, (6.004) tiadinil.

7)胺基酸及/或蛋白質生物合成之抑制劑，例如(7.001)賽普洛(cyprodinil)、(7.002)嘉賜黴素(kasugamycin)、(7.003)嘉賜黴素水合鹽酸鹽(kasugamycinhydrochloridehydrate)、(7.004)土黴素(oxytetracycline)、(7.005)派美尼(pyrimethanil)、(7.006)3-(5-氟-3,3,4,4-四甲基-3,4-二氫異喹啉-1-基)喹啉。 7) Inhibitors of amino acid and / or protein biosynthesis, such as (7.001) cyprodinil, (7.002) kasugamycin, (7.003) kasugamycin hydrochloridehydrate ), (7.004) oxytetracycline, (7.005) pirimethanil, (7.006) 3- (5-fluoro-3,3,4,4-tetramethyl-3,4-dihydro Isoquinolin-1-yl) quinoline.

8)ATP產生之抑制劑，例如(8.001)矽噻菌胺(silthiofam)。 8) Inhibitors of ATP production, such as (8.001) silthiofam.

9)細胞壁合成之抑制劑，例如(9.001)苯噻菌胺(benthiavalicarb)、(9.002)達滅芬(dimethomorph)、(9.003)氟嗎啉(flumorph)、(9.004)異丙菌胺(iprovalicarb)、(9.005)曼普胺(mandipropamid)、(9.006)吡嗎啉(pyrimorph)、(9.007)纈菌胺(valifenalate)、(9.008)(2E)-3-(4-第三丁基苯基)-3-(2-氯吡啶-4-基)-1-(嗎福啉-4-基)丙-2-烯-1-酮、(9.009)(2Z)-3-(4-第三丁基苯基)-3-(2-氯吡啶-4-基)-1-(嗎福啉-4-基)丙-2-烯-1-酮。 9) Inhibitors of cell wall synthesis, such as (9.001) benthiavalicarb, (9.002) dimethomorph, (9.003) flumorph, (9.004) iprovalicarb , (9.005) mandipropamid, (9.006) pyrimorph, (9.007) valifenalate, (9.008) (2E) -3- (4-third butylphenyl) -3- (2-chloropyridin-4-yl) -1- (morpholin-4-yl) prop-2-en-1-one, (9.009) (2Z) -3- (4-tert-butyl Phenyl) -3- (2-chloropyridin-4-yl) -1- (morpholin-4-yl) prop-2-en-1-one.

10)脂質和膜合成之抑制劑，例如(10.001)普拔克(propamocarb)、(10.002)普拔克鹽酸鹽(propamocarbhydrochloride)、(10.003)脫克松(tolclofos-methyl)。 10) Inhibitors of lipid and membrane synthesis, such as (10.001) propamocarb, (10.002) propamocarb hydrochloride, (10.003) tolclofos-methyl.

11)黑色素生物合成之抑制劑，例如(11.001)三賽唑(tricyclazole)、(11.002)2,2,2-三氟乙基{3-甲基-1-[(4-甲基苯甲醯基)胺基]丁-2-基}胺甲酸酯。 11) Inhibitors of melanin biosynthesis, such as (11.001) tricyclazole, (11.002) 2,2,2-trifluoroethyl {3-methyl-1-[(4-methylbenzidine ) Amino] but-2-yl} carbamate.

12)核酸合成抑制劑，例如(12.001)本達樂(benalaxyl)、(12.002)右本達樂(benalaxyl-M)(kiralaxyl)、(12.003)滅達樂(metalaxyl)、(12.004)右滅達樂(metalaxyl-M)(mefenoxam)。 12) Nucleic acid synthesis inhibitors, such as (12.001) benalaxyl, (12.002) benalaxyl-M, kiralaxyl, (12.003) metalaxyl, and (12.004) carbamidine Music (metalaxyl-M) (mefenoxam).

13)訊號轉導之抑制劑，例如(13.001)護汰寧(fludioxonil)、(13.002)依普同(iprodione)、(13.003)撲滅寧(procymidone)、(13.004)普快淨(proquinazid)、(13.005)快諾芬(quinoxyfen)、(13.006)免克寧(vinclozolin)。 13) Inhibitors of signal transduction, such as (13.001) fludioxonil, (13.002) iprodione, (13.003) procymidone, (13.004) proquinazid, ( 13.005) quinoxyfen, (13.006) vinclozolin.

14)作為去偶合劑的化合物，例如(14.001)扶吉胺(fluazinam)、(14.002)敵蟎普(meptyldinocap)。 14) A compound as a decoupling agent, for example, (14.001) fluazinam, (14.002) meptyldinocap.

15)其他化合物，例如(15.001)脫落酸(abscisicacid)、(15.002)苯噻硫氰(benthiazole)、(15.003)bethoxazin、(15.004)卡巴西黴素(capsimycin)、(15.005)香芹酮(carvone)、(15.006)蟎離丹(chinomethionat)、(15.007)硫雜靈(cufraneb)、(15.008)賽芬胺(cyflufenamid)、(15.009)克絕(cymoxanil)、(15.010)環丙磺醯胺(cyprosulfamide)、(15.011)flutianil、(15.012)福賽得-鋁(fosetyl-aluminium)、(15.013)福賽得-鈣(fosetyl-calcium)、(15.014)福賽得-鈉(fosetyl-sodium)、(15.015)異硫氰酸甲酯(methylisothiocyanate)、(15.016)滅芬農(metrafenon)、(15.017)米多黴素(mildiomycin)、(15.018)納他黴素(natamycin)、(15.019)二甲基二硫代胺甲酸鎳(nickeldimethyldithiocarbamate)、(15.020)酞菌酯(nitrothal-isopropyl)、(15.021)oxamocarb、(15.022)氟噻唑吡乙酮(oxathiapiprolin)、(15.023)oxyfenthiin、(15.024)五氯酚及其鹽、(15.025)膦酸及其鹽、(15.026)霜黴威乙膦酸鹽(propamocarb-fosetylate)、(15.027)pyriofenone(氯芬同(chlazafenone))、(15.028)異丁乙氧喹啉(tebufloquin)、(15.029)克枯爛(tecloftalam)、(15.030)甲磺菌胺(tolnifanide)、(15.031)1-(4-{4-[(5R)-5-(2,6-二氟苯基)-4,5-二氫-1,2-

Figure TW201945344A_D0090
唑-3-基]-1,3-噻唑-2-基}哌啶-1-基)-2-[5-甲基-3-(三氟甲基)-1H-吡唑-1-基]乙酮、(15.032)1-(4-{4-[(5S)-5-(2,6-二氟苯基)-4,5-二氫-1,2-
Figure TW201945344A_D0091
唑-3-基]-1,3-噻唑-2-基}哌啶-1-基)-2-[5-甲基-3-(三氟甲基)-1H-吡唑-1-基]乙酮、(15.033)2-(6-苯甲基吡啶-2-基)喹唑啉、(15.034)2,6-二甲基-1H,5H-[1,4]二硫雜環己烯并[2,3-c：5,6-c']二吡咯-1,3,5,7(2H,6H)-四酮、(15.035)2-[3,5-雙(二氟甲基)-1H-吡唑-1-基]-1-[4-(4-{5-[2-(丙-2-炔-1-基氧基)苯基]-4,5-二氫-1,2-
Figure TW201945344A_D0092
唑-3-基}-1,3-噻唑-2-基)哌啶-1-基]乙酮、(15.036)2-[3,5-雙(二氟甲基)-1H-吡唑-1-基]-1-[4-(4-{5-[2-氯-6-(丙-2-炔-1-基氧基)苯基]-4,5-二氫-1,2-
Figure TW201945344A_D0093
唑-3-基}-1,3-噻唑-2-基)哌啶-1-基]乙酮、(15.037)2-[3,5-雙(二氟甲基)-1H-吡唑-1-基]-1-[4-(4-{5-[2-氟-6-(丙-2-炔-1-基氧基)苯基]-4,5-二氫-1,2-
Figure TW201945344A_D0094
唑-3-基}-1,3-噻唑-2-基)哌啶-1-基]乙酮、(15.038)2-[6-(3-氟-4-甲氧基苯基)-5-甲 基吡啶-2-基]喹唑啉、(15.039)2-{(5R)-3-[2-(1-{[3,5-雙(二氟甲基)-1H-吡唑-1-基]乙醯基}哌啶-4-基)-1,3-噻唑-4-基]-4,5-二氫-1,2-
Figure TW201945344A_D0095
唑-5-基}-3-氯苯基甲磺酸酯、(15.040)2-{(5S)-3-[2-(1-{[3,5-雙(二氟甲基)-1H-吡唑-1-基]乙醯基}哌啶-4-基)-1,3-噻唑-4-基]-4,5-二氫-1,2-
Figure TW201945344A_D0096
唑-5-基}-3-氯苯基甲磺酸酯、(15.041)2-{2-[(7,8-二氟-2-甲基喹啉-3-基)氧基]-6-氟苯基}丙-2-醇、(15.042)2-{2-氟-6-[(8-氟-2-甲基喹啉-3-基)氧基]苯基}丙-2-醇、(15.043)2-{3-[2-(1-{[3,5-雙(二氟甲基)-1H-吡唑-1-基]乙醯基}哌啶-4-基)-1,3-噻唑-4-基]-4,5-二氫-1,2-
Figure TW201945344A_D0097
唑-5-基}-3-氯苯基甲磺酸酯、(15.044)2-{3-[2-(1-{[3,5-雙(二氟甲基)-1H-吡唑-1-基]乙醯基}哌啶-4-基)-1,3-噻唑-4-基]-4,5-二氫-1,2-
Figure TW201945344A_D0098
唑-5-基}苯基甲磺酸酯、(15.045)2-苯基酚及其鹽類、(15.046)3-(4,4,5-三氟-3,3-二甲基-3,4-二氫異喹啉-1-基)喹啉、(15.047)3-(4,4-二氟-3,3-二甲基-3,4-二氫異喹啉-1-基)喹啉、(15.048)4-胺基-5-氟嘧啶-2-醇(互變異構物形式：4-胺基-5-氟嘧啶-2(1H)-酮)、(15.049)4-側氧-4-[(2-苯基乙基)胺基]丁酸、(15.050)5-胺基-1,3,4-噻二唑-2-硫醇、(15.051)5-氯-N'-苯基-N'-(丙-2-炔-1-基)噻吩-2-磺醯肼、(15.052)5-氟-2-[(4-氟苯甲基)氧基]嘧啶-4-胺、(15.053)5-氟-2-[(4-甲基苯甲基)氧基]嘧啶-4-胺、(15.054)9-氟-2,2-二甲基-5-(喹啉-3-基)-2,3-二氫-1,4-苯并氮呯、(15.055)丁-3-炔-1-基{6-[({[(Z)-(1-甲基-1H-四唑-5-基)(苯基)伸甲基]胺基}氧基)甲基]吡啶-2-基}胺甲酸酯、(15.056)(2Z)-3-胺基-2-氰基-3-苯基丙烯酸乙酯、(15.057)啡
Figure TW201945344A_D0099
-1-羧酸、(15.058)3,4,5-三羥基苯甲酸丙酯、(15.059)喹啉-8-醇、(15.060)喹啉-8-醇硫酸酯(2：1)、(15.061)第三丁基{6-[({[(1-甲基-1H-四唑-5-基)(苯基)伸甲基]胺基}氧基)甲基]吡啶-2-基}胺甲酸酯、(15.062)5-氟-4-亞胺基-3-甲基-1-[(4-甲基苯基)磺醯基]-3,4-二氫嘧啶-2(1H)-酮、(15.063)metyltetraprole、(15.064)Aminopyrifen、(15.065)Pyrapropoyne、(15.066)(N'-[2-氯-4-(2-氟苯氧基)-5-甲基苯基]-N-乙基-N-甲基亞胺甲醯胺)、(15.067)(N'-(2-氯-5-甲基-4-苯氧基苯基)-N-乙基-N-甲基亞胺甲醯胺)、(15.068)(2-{2-[(7,8-二氟-2-甲基喹啉-3-基)氧基]-6-氟苯基}丙-2-醇)、(15.069)(5-溴-1-(5,6-二甲基吡啶-3-基)-3,3-二甲基-3,4-二氫異喹啉)、(15.070)(3-(4,4-二氟-5,5-二甲基-4,5-二氫 噻吩并[2,3-c]吡啶-7-基)喹啉)、(15.071)(1-(4,5-二甲基-1H-苯并咪唑-1-基)-4,4-二氟-3,3-二甲基-3,4-二氫異喹啉)、(15.072)8-氟-3-(5-氟-3,3-二甲基-3,4-二氫異喹啉-1-基)喹若酮、(15.073)8-氟-3-(5-氟-3,3,4,4-四甲基-3,4-二氫異喹啉-1-基)喹若酮、(15.074)3-(4,4-二氟-3,3-二甲基-3,4-二氫異喹啉-1-基)-8-氟喹啉、(15.075)(N-甲基-N-苯基-4-[5-(三氟甲基)-1,2,4-
Figure TW201945344A_D0100
二唑-3-基]苯甲醯胺)、(15.076)({4-[5-(三氟甲基)-1,2,4-
Figure TW201945344A_D0101
二唑-3-基]苯基}胺甲酸甲酯)、(15.077)(N-{4-[5-(三氟甲基)-1,2,4-
Figure TW201945344A_D0102
二唑-3-基]苯甲基}環丙甲醯胺)、(15.078)N-甲基-4-(5-(三氟甲基)-1,2,4-
Figure TW201945344A_D0103
二唑-3-基]苯甲醯胺、(15.079)N-[(E)-甲氧基亞胺基甲基]-4-[5-(三氟甲基)-1,2,4-
Figure TW201945344A_D0104
二唑-3-基]苯甲醯胺、(15.080)N-[(Z)-甲氧基亞胺基甲基]-4-[5-(三氟甲基)-1,2,4-
Figure TW201945344A_D0105
二唑-3-基]苯甲醯胺、(15.081)N-[4-[5-(三氟甲基)-1,2,4-
Figure TW201945344A_D0106
二唑-3-基]苯基]環丙甲醯胺、(15.082)N-(2-氟苯基)-4-[5-(三氟甲基)-1,2,4-
Figure TW201945344A_D0107
二唑-3-基]苯甲醯胺、(15.083)2,2-二氟-N-甲基-2-[4-[5-(三氟甲基)-1,2,4-
Figure TW201945344A_D0108
二唑-3-基]苯基]乙醯胺、(15.084)N-烯丙基-N-[[4-[5-(三氟甲基)-1,2,4-
Figure TW201945344A_D0109
二唑-3-基)苯基]甲基]乙醯胺、(15.085)N-[(E)-N-甲氧基-C-甲基-伸亞胺醯基]-4-(5-(三氟甲基)-1,2,4-
Figure TW201945344A_D0110
二唑-3-基]苯甲醯胺、(15.086)N-[(Z)-N-甲氧基-C-甲基-伸亞胺醯基]-4-[5-(三氟甲基)-1,2,4-
Figure TW201945344A_D0111
二唑-3-基]苯甲醯胺、(15.087)N-烯丙基-N-[[4-[5-(三氟甲基)-1,2,4-
Figure TW201945344A_D0112
二唑-3-基]苯基]甲基]丙醯胺、(15.088)4,4-二甲基-1-[[4-[5-(三氟甲基)-1,2,4-
Figure TW201945344A_D0113
二唑-3-基]苯基]甲基]吡咯啶-2-酮、(15.089)N-甲基-4-[5-(三氟甲基)-1,2,4-
Figure TW201945344A_D0114
二唑-3-基]硫代苯甲醯胺、(15.090)5-甲基-1-[[4-[5-(三氟甲基)-1,2,4-
Figure TW201945344A_D0115
二唑-3-基]苯基]甲基]吡咯啶-2-酮、(15.091)N-((2,3-二氟-4-[5-(三氟甲基)-1,2,4-
Figure TW201945344A_D0116
二唑-3-基]苯基]甲基]-3,3,3-三氟-丙醯胺、(15.092)1-甲氧基-1-甲基-3-[[4-[5-(三氟甲基}-1,2,4-
Figure TW201945344A_D0117
二唑-3-基]苯基]甲基]脲、(15.093)1,1-二乙基-3-[[4-[5-(三氟甲基}-1,2,4-
Figure TW201945344A_D0118
二唑-3-基]苯基]甲基]脲、(15.094)N-[[4-[5-(三氟甲基)-1,2,4-
Figure TW201945344A_D0119
二唑-3-基]苯-基)甲基)丙醯胺、(15.095)N-甲氧基-N-[[4-[5-(三氟甲基)-1,2,4-
Figure TW201945344A_D0120
二唑-3-基]苯基]甲基]環丙甲醯胺、(15.096)1-甲氧基-3-甲基-1-[[4-[5-(三氟甲基)-1,2,4-
Figure TW201945344A_D0121
二唑-3-基]苯基]甲基]脲、(15.097)N-甲氧基-N-[[4-[5-(三氟甲基)-1,2,4-
Figure TW201945344A_D0122
二唑-3-基]苯基]甲基)環 丙甲醯胺；(15.098)N,2-二甲氧基-N-[[4-[5-(三氟甲基}-1,2,4-
Figure TW201945344A_D0123
二唑-3-基]苯基]甲基]丙醯胺、(15.099)N-乙基-2-甲基-N-[[4-[5-(三氟甲基)-1,2,4-
Figure TW201945344A_D0124
二唑-3-基)苯基]甲基丙醯胺、(15.100)1-甲氧基-3-甲基-1-[[4-[5-(三氟甲基)-1,2,4-
Figure TW201945344A_D0125
二唑-3-基]苯基]甲基]脲、(15.101)1,3-二甲氧基-1-[[4-[5-(三氟甲基)-1,2,4-
Figure TW201945344A_D0126
二唑-3-基]苯基]甲基]脲、(15.102)3-乙基-1-甲氧基-1-[[4-[5-(三氟甲基)-1,2,4-
Figure TW201945344A_D0127
二唑-3-基]苯基]甲基]脲、(15.103)1-[[4-[5-(三氟甲基)-1,2、4-
Figure TW201945344A_D0128
二唑-3-基]苯基]甲基]哌啶-2-酮、(15.104)4,4-二甲基-2-[[4-(5-(三氟甲基)-1,2,4-
Figure TW201945344A_D0129
二唑-3-基]苯基]甲基]異
Figure TW201945344A_D0130
唑啶-3-酮、(15.105)5,5-二甲基-2-[[4-[5-(三氟甲基)-1,2,4-
Figure TW201945344A_D0131
二唑-3-基]苯基]甲基]異
Figure TW201945344A_D0132
唑啶-3-酮、(15.106)、3,3-二甲基-1-[[4-[5-(三氟甲基)-1,2,4-
Figure TW201945344A_D0133
二唑-3-基]苯基]甲基[哌啶-2-酮、(15.107)1-[[3-氟-4-(5-(三氟甲基)-1,2,4-
Figure TW201945344A_D0134
二唑-3-基]苯基]甲基]氮
Figure TW201945344A_D0135
-2-酮、(15.108)4,4-二甲基-2-[[4-(5-(三氟甲基)-1,2,4-
Figure TW201945344A_D0136
二唑-3-基]苯基]甲基]異
Figure TW201945344A_D0137
唑啶-3-酮及(15.109)5,5-二甲基-2-[[4-[5-(三氟甲基)-1,2,4-
Figure TW201945344A_D0138
二唑-3-基]苯基]甲基]異
Figure TW201945344A_D0139
唑啶-3-酮。 15) Other compounds, such as (15.001) abscisicacid, (15.002) benthiazole, (15.003) bethoxazin, (15.004) capsimycin, (15.005) carvone ), (15.006) chinomethionat, (15.007) cufraneb, (15.008) cyflufenamid, (15.009) cymoxanil, (15.010) ciproflamine (15.010) cyprosulfamide), (15.011) flutianil, (15.012) forsetyl-aluminium, (15.013) forsetyl-calcium, (15.014) forsetyl-sodium, (15.015) methylisothiocyanate, (15.016) metrafenon, (15.017) mildomycin, (15.018) natamycin, (15.019) dimethyl Nickeldimethyldithiocarbamate, (15.020) nitrothal-isopropyl, (15.021) oxamocarb, (15.022) oxathiapiprolin, (15.023) oxyfenthiin, (15.024) pentachloro Phenol and its salts, (15.025) phosphonic acid and its salts, (15.026) propamocarb-fosetylate, (15.027) pyriofenone (chlorofen with (chlaza fenone)), (15.028) tebufloquin, (15.029) tecloftalam, (15.030) tolnifanide, (15.031) 1- (4- (4- ( (5R) -5- (2,6-difluorophenyl) -4,5-dihydro-1,2-
Figure TW201945344A_D0090
Azol-3-yl] -1,3-thiazol-2-yl} piperidin-1-yl) -2- [5-methyl-3- (trifluoromethyl) -1H-pyrazol-1-yl ] Ethyl ketone, (15.032) 1- (4- {4-[(5S) -5- (2,6-difluorophenyl) -4,5-dihydro-1,2-
Figure TW201945344A_D0091
Azol-3-yl] -1,3-thiazol-2-yl} piperidin-1-yl) -2- [5-methyl-3- (trifluoromethyl) -1H-pyrazol-1-yl ] Ethyl ketone, (15.033) 2- (6-benzylpyridin-2-yl) quinazoline, (15.034) 2,6-dimethyl-1H, 5H- [1,4] dithiacyclohexane Eno [2,3-c: 5,6-c '] dipyrrole-1,3,5,7 (2H, 6H) -tetraone, (15.035) 2- [3,5-bis (difluoromethyl) ) -1H-pyrazol-1-yl] -1- [4- (4- {5- [2- (prop-2-yn-1-yloxy) phenyl] -4,5-dihydro -1,2-
Figure TW201945344A_D0092
Azole-3-yl} -1,3-thiazol-2-yl) piperidin-1-yl] ethanone, (15.036) 2- [3,5-bis (difluoromethyl) -1H-pyrazole- 1-yl] -1- [4- (4- {5- [2-chloro-6- (prop-2-yn-1-yloxy) phenyl] -4,5-dihydro-1,2 -
Figure TW201945344A_D0093
Azole-3-yl} -1,3-thiazol-2-yl) piperidin-1-yl] ethanone, (15.037) 2- [3,5-bis (difluoromethyl) -1H-pyrazole- 1-yl] -1- [4- (4- {5- [2-fluoro-6- (prop-2-yn-1-yloxy) phenyl] -4,5-dihydro-1,2 -
Figure TW201945344A_D0094
Azol-3-yl} -1,3-thiazol-2-yl) piperidin-1-yl] ethanone, (15.038) 2- [6- (3-fluoro-4-methoxyphenyl) -5 -Methylpyridin-2-yl] quinazoline, (15.039) 2-{(5R) -3- [2- (1-{[3,5-bis (difluoromethyl) -1H-pyrazole- 1-yl] ethenyl} piperidin-4-yl) -1,3-thiazol-4-yl] -4,5-dihydro-1,2-
Figure TW201945344A_D0095
Azol-5-yl} -3-chlorophenylmethanesulfonate, (15.040) 2-{(5S) -3- [2- (1-{[3,5-bis (difluoromethyl) -1H -Pyrazol-1-yl] ethenyl} piperidin-4-yl) -1,3-thiazol-4-yl] -4,5-dihydro-1,2-
Figure TW201945344A_D0096
Azol-5-yl} -3-chlorophenylmethanesulfonate, (15.041) 2- {2-[(7,8-difluoro-2-methylquinolin-3-yl) oxy] -6 -Fluorophenyl} propan-2-ol, (15.042) 2- {2-fluoro-6-[(8-fluoro-2-methylquinolin-3-yl) oxy] phenyl} propan-2- Alcohol, (15.043) 2- {3- [2- (1-([3,5-bis (difluoromethyl) -1H-pyrazol-1-yl] ethenyl} piperidin-4-yl) -1,3-thiazol-4-yl] -4,5-dihydro-1,2-
Figure TW201945344A_D0097
Azol-5-yl} -3-chlorophenylmethanesulfonate, (15.044) 2- {3- [2- (1-{[3,5-bis (difluoromethyl) -1H-pyrazole- 1-yl] ethenyl} piperidin-4-yl) -1,3-thiazol-4-yl] -4,5-dihydro-1,2-
Figure TW201945344A_D0098
Azol-5-yl} phenyl methanesulfonate, (15.045) 2-phenylphenol and its salts, (15.046) 3- (4,4,5-trifluoro-3,3-dimethyl-3 , 4-dihydroisoquinolin-1-yl) quinoline, (15.047) 3- (4,4-difluoro-3,3-dimethyl-3,4-dihydroisoquinolin-1-yl ) Quinoline, (15.048) 4-amino-5-fluoropyrimidin-2-ol (tautomer form: 4-amino-5-fluoropyrimidin-2 (1H) -one), (15.049) 4- Pendant oxygen-4-[(2-phenylethyl) amino] butanoic acid, (15.050) 5-amino-1,3,4-thiadiazole-2-thiol, (15.051) 5-chloro- N'-phenyl-N '-(prop-2-yn-1-yl) thiophene-2-sulfohydrazine, (15.052) 5-fluoro-2-[(4-fluorobenzyl) oxy] pyrimidine -4-amine, (15.053) 5-fluoro-2-[(4-methylbenzyl) oxy] pyrimidin-4-amine, (15.054) 9-fluoro-2,2-dimethyl-5- (Quinolin-3-yl) -2,3-dihydro-1,4-benzoazepine, (15.055) but-3-yn-1-yl {6-[({[(((Z)-(1 -Methyl-1H-tetrazol-5-yl) (phenyl) methylene] amino} oxy) methyl] pyridin-2-yl} carbamate, (15.056) (2Z) -3- Ethyl-2-cyano-3-phenyl acrylate, (15.057) morphine
Figure TW201945344A_D0099
1-carboxylic acid, (15.058) propyl 3,4,5-trihydroxybenzoate, (15.059) quinoline-8-ol, (15.060) quinoline-8-alcohol sulfate (2: 1), ( 15.061) Third butyl {6-[({(((1-methyl-1H-tetrazol-5-yl) (phenyl) methylidene) amino} oxy) methyl] pyridin-2-yl } Carbamate, (15.062) 5-fluoro-4-imino-3-methyl-1-[(4-methylphenyl) sulfonamido] -3,4-dihydropyrimidine-2 ( 1H) -one, (15.063) metyltetraprole, (15.064) Aminopyrifen, (15.065) Pyrapropoyne, (15.066) (N '-[2-chloro-4- (2-fluorophenoxy) -5-methylphenyl] -N-ethyl-N-methylimine formamidine), (15.067) (N '-(2-chloro-5-methyl-4-phenoxyphenyl) -N-ethyl-N- Methylimine formamidine), (15.068) (2- {2-[(7,8-difluoro-2-methylquinolin-3-yl) oxy] -6-fluorophenyl} propane- 2-alcohol), (15.069) (5-bromo-1- (5,6-dimethylpyridin-3-yl) -3,3-dimethyl-3,4-dihydroisoquinoline), ( 15.070) (3- (4,4-difluoro-5,5-dimethyl-4,5-dihydrothieno [2,3-c] pyridin-7-yl) quinoline), (15.071) ( 1- (4,5-dimethyl-1H-benzimidazol-1-yl) -4,4-difluoro-3,3-dimethyl-3,4-dihydroisoquinoline), (15.072 ) 8-fluoro-3- (5-fluoro-3,3-dimethyl-3,4-dihydroisoquinolin-1-yl) quinazinone, (15.0 73) 8-fluoro-3- (5-fluoro-3,3,4,4-tetramethyl-3,4-dihydroisoquinolin-1-yl) quinoxone, (15.074) 3- (4 , 4-difluoro-3,3-dimethyl-3,4-dihydroisoquinolin-1-yl) -8-fluoroquinoline, (15.075) (N-methyl-N-phenyl-4 -[5- (trifluoromethyl) -1,2,4-
Figure TW201945344A_D0100
Diazol-3-yl] benzamidine), (15.076) ((4- [5- (trifluoromethyl) -1,2,4-
Figure TW201945344A_D0101
Diazol-3-yl] phenyl} carbamate), (15.077) (N- {4- [5- (trifluoromethyl) -1,2,4-
Figure TW201945344A_D0102
Diazol-3-yl] benzyl} cyclopropylmethanamine), (15.078) N-methyl-4- (5- (trifluoromethyl) -1,2,4-
Figure TW201945344A_D0103
Diazol-3-yl] benzidine, (15.079) N-[(E) -methoxyiminomethyl] -4- [5- (trifluoromethyl) -1,2,4-
Figure TW201945344A_D0104
Diazol-3-yl] benzamide, (15.080) N-[(Z) -methoxyiminomethyl] -4- [5- (trifluoromethyl) -1,2,4-
Figure TW201945344A_D0105
Diazol-3-yl] benzidine, (15.081) N- [4- [5- (trifluoromethyl) -1,2,4-
Figure TW201945344A_D0106
Diazol-3-yl] phenyl] cyclopropylmethanamine, (15.082) N- (2-fluorophenyl) -4- [5- (trifluoromethyl) -1,2,4-
Figure TW201945344A_D0107
Diazol-3-yl] benzidine, (15.083) 2,2-difluoro-N-methyl-2- [4- [5- (trifluoromethyl) -1,2,4-
Figure TW201945344A_D0108
Diazol-3-yl] phenyl] acetamidamine, (15.084) N-allyl-N-[[4- [5- (trifluoromethyl) -1,2,4-
Figure TW201945344A_D0109
Diazol-3-yl) phenyl] methyl] acetamidinium, (15.085) N-[(E) -N-methoxy-C-methyl-iminofluorenyl] -4- (5- (Trifluoromethyl) -1,2,4-
Figure TW201945344A_D0110
Diazol-3-yl] benzamidine, (15.086) N-[(Z) -N-methoxy-C-methyl-iminofluorenyl] -4- [5- (trifluoromethyl ) -1,2,4-
Figure TW201945344A_D0111
Diazol-3-yl] benzidine, (15.087) N-allyl-N-[[4- [5- (trifluoromethyl) -1,2,4-
Figure TW201945344A_D0112
Diazol-3-yl] phenyl] methyl] propanamide, (15.088) 4,4-dimethyl-1-[[4- [5- (trifluoromethyl) -1,2,4-
Figure TW201945344A_D0113
Diazol-3-yl] phenyl] methyl] pyrrolidin-2-one, (15.089) N-methyl-4- [5- (trifluoromethyl) -1,2,4-
Figure TW201945344A_D0114
Diazol-3-yl] thiobenzidine, (15.090) 5-methyl-1-[[4- [5- (trifluoromethyl) -1,2,4-
Figure TW201945344A_D0115
Diazol-3-yl] phenyl] methyl] pyrrolidin-2-one, (15.091) N-((2,3-difluoro-4- [5- (trifluoromethyl) -1,2, 4-
Figure TW201945344A_D0116
Diazol-3-yl] phenyl] methyl] -3,3,3-trifluoro-propanamide, (15.092) 1-methoxy-1-methyl-3-[[4- [5- (Trifluoromethyl) -1,2,4-
Figure TW201945344A_D0117
Diazol-3-yl] phenyl] methyl] urea, (15.093) 1,1-diethyl-3-[[4- [5- (trifluoromethyl) -1,2,4-
Figure TW201945344A_D0118
Diazol-3-yl] phenyl] methyl] urea, (15.094) N-[[4- [5- (trifluoromethyl) -1,2,4-
Figure TW201945344A_D0119
Diazol-3-yl] benzene-yl) methyl) propanamide, (15.095) N-methoxy-N-[[4- [5- (trifluoromethyl) -1,2,4-
Figure TW201945344A_D0120
Diazol-3-yl] phenyl] methyl] cyclopropylmethanamine, (15.096) 1-methoxy-3-methyl-1-[[4- [5- (trifluoromethyl) -1 , 2,4-
Figure TW201945344A_D0121
Diazol-3-yl] phenyl] methyl] urea, (15.097) N-methoxy-N-[[4- [5- (trifluoromethyl) -1,2,4-
Figure TW201945344A_D0122
Diazol-3-yl] phenyl] methyl) cyclopropylmethanamine; (15.098) N, 2-dimethoxy-N-[[4- [5- (trifluoromethyl) -1,2 , 4-
Figure TW201945344A_D0123
Diazol-3-yl] phenyl] methyl] propanamide, (15.099) N-ethyl-2-methyl-N-[[4- [5- (trifluoromethyl) -1,2, 4-
Figure TW201945344A_D0124
Diazol-3-yl) phenyl] methylpropanamide, (15.100) 1-methoxy-3-methyl-1-[[4- [5- (trifluoromethyl) -1,2, 4-
Figure TW201945344A_D0125
Diazol-3-yl] phenyl] methyl] urea, (15.101) 1,3-dimethoxy-1-[[4- [5- (trifluoromethyl) -1,2,4-
Figure TW201945344A_D0126
Diazol-3-yl] phenyl] methyl] urea, (15.102) 3-ethyl-1-methoxy-1-[[4- [5- (trifluoromethyl) -1,2,4 -
Figure TW201945344A_D0127
Diazol-3-yl] phenyl] methyl] urea, (15.103) 1-[[4- [5- (trifluoromethyl) -1,2,4-
Figure TW201945344A_D0128
Diazol-3-yl] phenyl] methyl] piperidin-2-one, (15.104) 4,4-dimethyl-2-[[4- (5- (trifluoromethyl) -1,2 , 4-
Figure TW201945344A_D0129
Diazol-3-yl] phenyl] methyl] iso
Figure TW201945344A_D0130
Amidazin-3-one, (15.105) 5,5-dimethyl-2-[[4- [5- (trifluoromethyl) -1,2,4-
Figure TW201945344A_D0131
Diazol-3-yl] phenyl] methyl] iso
Figure TW201945344A_D0132
Oxazidin-3-one, (15.106), 3,3-dimethyl-1-[[4- [5- (trifluoromethyl) -1,2,4-
Figure TW201945344A_D0133
Diazol-3-yl] phenyl] methyl [piperidin-2-one, (15.107) 1-[[3-fluoro-4- (5- (trifluoromethyl) -1,2,4-
Figure TW201945344A_D0134
Diazol-3-yl] phenyl] methyl] nitrogen
Figure TW201945344A_D0135
-2-one, (15.108) 4,4-dimethyl-2-[[4- (5- (trifluoromethyl) -1,2,4-
Figure TW201945344A_D0136
Diazol-3-yl] phenyl] methyl] iso
Figure TW201945344A_D0137
Amidazin-3-one and (15.109) 5,5-dimethyl-2-[[4- [5- (trifluoromethyl) -1,2,4-
Figure TW201945344A_D0138
Diazol-3-yl] phenyl] methyl] iso
Figure TW201945344A_D0139
Amidazin-3-one.

所有如上文所述之(1)至(15)類的名稱混合項目可以游離的化合物及/或，若其功能基團可行的話，其農業上可接受鹽存在。 All of the above-named (1) to (15) mixed name items may be free compounds and / or, if their functional groups are feasible, their agriculturally acceptable salts are present.

本發明之化合物和組成物亦可與一或多種生物防治劑組合。 The compounds and compositions of the present invention may also be combined with one or more biological control agents.

可與本發明之化合物和組成物組合之生物控制劑的實例有：(A)由下列組成之群中選出的抗細菌劑：(A1)細菌，例如(A1.1)枯草芽孢桿菌(Bacillus subtilis)，特別是QST713/AQ713菌株(可取得的為SERENADE OPTI或SERENADE ASO，來自Bayer CropScience LP,US，具有NRRL登錄號B21661及如美國專利第6,060,051號中所述)；(A1.2)液化澱粉芽孢桿菌(Bacillus amyloliquefaciens)，特別是D747菌株(可取得的為Double NickelTM，來自Certis,US具有登錄號FERM BP-8234及揭示於美國專利第7,094,592號)；(A1.3)短小芽孢桿菌(Bacillus pumilus)，特別是BU F-33菌株(具有NRRL登錄號50185)；(A1.4)液化澱粉枯草芽孢桿菌變種(Bacillus subtilis var.amyloliquefaciens)FZB24菌株(可取得的為Taegro®，來自Novozymes,US)； (A1.5)類芽孢桿菌屬(Paenibacillus sp.)具有登錄號NRRL B-50972或登錄號NRRL B-67129菌株及描述於國際專利申請案第WO 2016/154297號；及(A2)真菌，例如(A2.1)出芽短梗黴菌(Aureobasidium pullulans)，特別是DSM14940菌株的芽生孢子；(A2.2)出芽短梗黴菌，DSM 14941菌株的芽生孢子；(A2.3)出芽短梗黴菌，特別是菌株DSM14940和DSM14941之芽生孢子混合物；(B)由下列組成之群中選出的殺真菌劑：(B1)細菌，例如(B1.1)枯草芽孢桿菌(Bacillus subtilis)，特別是QST713/AQ713菌株(可取得的為SERENADE OPTI或SERENADE ASO，來自Bayer CropScience LP,US，具有NRRL登錄號B21661及如美國專利第6,060,051號中所述；(B1.2)短小芽孢桿菌，特別是QST2808菌株(可取得的為SONATA®，來自Bayer CropScience LP,US，具有登錄號NRRL B-30087及如美國專利第6,245,551號中所述)；(B1.3)短小芽孢桿菌，特別是GB34菌株(可取得的為Yield Shield®，來自Bayer AG,DE)；(B1.4)短小芽孢桿菌，特別是BU F-33菌株(具有NRRL登錄號50185)；(B1.5)液化澱粉芽孢桿菌，特別是D747菌株(可取得的為Double NickelTM，來自Certis,US，具有登錄號FERM BP-8234及揭示於美國專利第7,094,592號)；(B1.6)枯草芽孢桿菌Y1336(可取得的為BIOBAC® WP，來自Bion-Tech,Taiwan，在台灣註冊為生物殺真菌劑，註冊號4764,5454、5096和5277)；(B1.7)液化澱粉芽孢桿菌MBI 600菌株(可取得的為SUBTILEX from BASF SE)；(B1.8)枯草芽孢桿菌GB03菌株(可取得的為Kodiak®，來自Bayer AG,DE)；(B1.9)液化澱粉枯草芽孢桿菌變種FZB24菌株(可來自Novozymes Biologicals Inc.,Salem,Virginia或Syngenta Crop Protection,LLC,Greensboro,North Carolina為殺真菌劑TAEGRO®或TAEGRO® ECO(EPA註冊號70127-5)；(B1.10)蕈狀芽孢桿菌(Bacillus mycoides)分離株J(可取得的為BmJ TGAI或WG，來自Certis USA)；(B1.11)地衣芽孢桿菌(Bacillus licheniformis)，特別是SB3086菌株(可取得的為EcoGuard TM Biofungicide和Green Releaf，來自Novozymes)； (B1.12)具有登錄號NRRL B-50972或登錄號NRRL B-67129之類芽孢桿菌屬菌株並描述於國際專利申請案第WO 2016/154297號。 Examples of biological control agents that can be combined with the compounds and compositions of the present invention are: (A) antibacterial agents selected from the group consisting of: (A1) bacteria, such as (A1.1) Bacillus subtilis ), Especially QST713 / AQ713 strains (available as SERENADE OPTI or SERENADE ASO from Bayer CropScience LP, US, with NRRL accession number B21661 and as described in US Patent No. 6,060,051); (A1.2) Liquefied starch Bacillus amyloliquefaciens , especially D747 strain (available as Double Nickel ™ , from Certis, US with accession number FERM BP-8234 and disclosed in US Patent No. 7,094,592); (A1.3) Bacillus pumilus ( Bacillus pumilus ), especially BU F-33 strain (with NRRL accession number 50185); (A1.4) Liquefied starch Bacillus subtilis variant ( Bacillus subtilis var.amyloliquefaciens ) strain FZB24 (available as Taegro®, from Novozymes, US); (A1.5) Paenibacillus sp. Strains having accession number NRRL B-50972 or accession number NRRL B-67129 and described in International Patent Application No. WO 2016/154297; and (A2) Fungi such as ( A2.1) Aureobasidium pullulans , especially the spores of DSM14940 strain; (A2.2) Spores germinating, DSM 14941 strains; (A2.3) Spores germinating, especially Spore mixtures of strains DSM14940 and DSM14941; (B) fungicides selected from the group consisting of: (B1) bacteria, such as (B1.1) Bacillus subtilis , especially QST713 / AQ713 strains ( Available are SERENADE OPTI or SERENADE ASO from Bayer CropScience LP, US, with NRRL accession number B21661 and as described in US Patent No. 6,060,051; (B1.2) Bacillus pumilus, especially QST2808 strain (available SONATA®, from Bayer CropScience LP, US, with accession number NRRL B-30087 and as described in US Patent No. 6,245,551; (B1.3) Bacillus pumilus, especially GB34 strain (available as Yield Shield ® from Bayer AG, DE); (B1.4) Bacillus pumilus, especially BU F-33 strain (with NRRL accession number 50185); (B1.5) Bacillus amyloliquefaciens, especially D747 strain (available from for the Double Nickel TM, from Certis, US Having the accession number FERM BP-8234 and disclosed in U.S. Patent No. 7,094,592); (B1.6) Bacillus subtilis Y1336 (that can be acquired as BIOBAC ® WP, from Bion-Tech, Taiwan, registered biological fungicide Taiwan (Registration Nos. 4764, 5454, 5096 and 5277); (B1.7) Bacillus amyloliquefaciens MBI 600 strain (available as SUBTILEX from BASF SE); (B1.8) Bacillus subtilis GB03 strain (available as Kodiak® from Bayer AG, DE); (B1.9) Liquefied starch Bacillus subtilis variant FZB24 strain (available from Novozymes Biologicals Inc., Salem, Virginia or Syngenta Crop Protection, LLC, Greensboro, North Carolina is a fungicide TAEGRO ® or TAEGRO ® ECO (EPA registration number 70127-5); (B1.10) Bacillus mycoides isolate J (available as BmJ TGAI or WG from Certis USA); (B1.11) Bacillus licheniformis , especially SB3086 strains (available as EcoGuard ™ Biofungicide and Green Releaf from Novozymes); (B1.12) with spore-like spores like NRRL B-50972 or NRRL B-67129 Bacillus strains and described in international patent application No. WO 2016/154297.

在某些具體實例中，生物防治劑為產生豐原素(fengycin)或巴斯他汀型(plipastatin-type)化合物、伊枯草菌素型(iturin-type)化合物及/或表面素型(surfactin-type)化合物之枯草芽孢桿菌或液化澱粉芽孢桿菌菌株。就背景，請參見下列評論文章：Ongena,M.,et al.,“Bacillus Lipopeptides：Versatile Weapons for Plant Disease Biocontrol,”Trends in Microbiology,Vol 16,No.3,March 2008,pp.115-125。能產生脂肽的芽孢桿菌菌株包括枯草芽孢桿菌QST713(可取得的為SERENADE OPTI或SERENADE ASO，來自Bayer CropScience LP,US，具有NRRL登錄號B21661及描述於美國專利第6,060,051號)、液化澱粉芽孢桿菌D747菌株(可取得的為Double NickelTM，來自Certis,US，具有登錄號FERM BP-8234及描述於美國專利第7,094,592號)；枯草芽孢桿菌MBI600(可取得的為SUBTILEX®，來自Becker Underwood,US EPA註冊號71840-8)；枯草芽孢桿菌Y1336(可取得的為BIOBAC® WP，來自Bion-Tech,Taiwan，在台灣註冊為生物殺真菌劑，註冊號4764、5454、5096和5277)；液化澱粉芽孢桿菌，特別是FZB42菌株(可取得的為RHIZOVITAL®，來自ABiTEP,DE)；以及液化澱粉枯草芽孢桿菌變種FZB24(可得自Novozymes Biologicals Inc.,Salem,Virginia或Syngenta Crop Protection,LLC,Greensboro,North Carolina為殺真菌劑TAEGRO®或TAEGRO® ECO(EPA註冊號70127-5)；及(B2)真菌，例如：(B2.1)微坦盾殼黴(Coniothyrium minitans)，特別是CON/M/91-8菌株(登錄號DSM-9660；例如來自Bayer的Contans®)；(B2.2)梅奇酵母菌(Metschnikowia fructicola)，特別是NRRL Y-30752菌株(例如Shemer®)；(B2.3)黃褐小球殼孢菌(Microsphaeropsis ochracea)(例如來自Prophyta的Microx®)；(B2.5)木黴菌屬(Trichoderma spp.)，包括深綠木黴菌(Trichoderma atroviride)，描述於國際專利申請案號PCT/IT2008/000196的SC1菌株)；(B2.6)哈氏木黴菌(Trichoderma harzianum rifai)KRL-AG2菌株(液稱為T-22菌株，/ATCC 208479，例如PLANTSHIELD T-22G,Rootshield® 和TurfShield，來自BioWorks,US)；(B2.14)粉紅黏帚黴(Gliocladium roseum)，321U菌株，來自W.F.Stoneman Company LLC；(B2.35)黃色籃狀菌(Talaromyces flavus)，V117b菌株；(B2.36)棘孢木黴菌(Trichoderma asperellum)，ICC 012菌株，來自Isagro；(B2.37)棘孢木黴菌SKT-1菌株(例如ECO-HOPE®，來自Kumiai Chemical Industry)；(B2.38)深綠木黴菌CNCM I-1237菌株(例如Esquive® WP，來自Agrauxine,FR)；(B2.39)深綠木黴菌菌株編號V08/002387；(B2.40)深綠木黴菌菌株NMI編號V08/002388；(B2.41)深綠木黴菌菌株NMI編號V08/002389；(B2.42)深綠木黴菌菌株NMI編號V08/002390；(B2.43)深綠木黴菌菌株LC52(例如Agrimm Technologies Limited公司之Tenet)；(B2.44)深綠木黴菌菌株ATCC 20476(IMI 206040)；(B2.45)深綠木黴菌菌株T11(IMI352941/CECT20498)；(B2.46)鉤狀木黴菌(Trichoderma harmatum)；(B2.47)鉤狀木黴菌；(B2.48)哈氏木黴菌T39(例如來自Makhteshim,US之Trichodex®)；(B2.49)哈氏木黴菌，特別是KD菌株(例如Trichoplus，來自Biological Control Products,SA(由Becker Underwood取得))；(B2.50)哈氏木黴菌ITEM 908菌株(例如來自Koppert之Trianum-P)；(B2.51)哈氏木黴菌TH35菌株(例如Mycontrol之Root-Pro)；(B2.52)綠木黴菌(Trichoderma virens)(亦稱為青綠黏帚黴(Gliocladium virens))，特別是GL-21菌株(例如Certis US之SoilGard 12G)；(B2.53)綠木黴菌(Trichoderma viride)，TV1菌株(例如Koppert之Trianum-P)；(B2.54)白粉寄生菌(Ampelomyces quisqualis)，特別是AQ 10菌株(例如IntrachemBio Italia之AQ 10®)；(B2.56)出芽短梗黴菌，特別是DSM14940菌株的芽生胞子；(B2.57)出芽短梗黴菌，特別是DSM 14941菌株的芽生孢子；(B2.58)出芽短梗黴菌，特別是DSM14940和DSM 14941菌株的芽生孢子(例如bio-ferm,CH之Botector®)；(B2.64)芽枝狀枝孢菌(Cladosporium cladosporioides)，H39菌株(來自Stichting Dienst Landbouwkundig Onderzoek)；(B2.69)鏈孢黏帚黴(Gliocladium catenulatum)(同物異名：粉紅黏帚黴(Clonostachys rosea f.catenulate)J1446菌株(例如AgBio Inc.之Prestop ®以及例如Kemira Agro Oy之Primastop®)；(B2.70)蠟蚧輪枝菌(Lecanicillium lecanii)(以前稱為Verticillium lecanii conidia)之KV01菌株(例如Koppert/Arysta之Vertalec®)；(B2.71)蠕形青黴菌(Penicillium vermiculatum)；(B2.72)異常畢赤酵母(Pichia anomala)WRL-076菌株(NRRL Y-30842)；(B2.75)深綠木黴菌SKT-1菌株(FERM P-16510)；(B2.76)深綠木黴菌SKT-2菌株(FERM P-16511)；(B2.77)深綠木黴菌SKT-3菌株(FERM P-17021)；(B2.78)蓋姆斯木黴菌(Trichoderma gamsii)(以前T.viride)ICC080菌株(IMI CC 392151 CABI，例如AGROBIOSOL DE MEXICO,S.A.DE C.V.之BioDerma)；(B2.79)哈氏木黴菌DB 103菌株(例如Dagutat Biolab之T-Gro 7456)；(B2.80)多孢木黴菌(Trichoderma polysporum)IMI 206039菌株(例如BINAB Bio-Innovation AB,Sweden之Binab TF WP)；(B2.81)子座木黴菌(Trichoderma stromaticum)(例如Ceplac,Brazil之Tricovab)；(B2.83)奧德曼細基格孢菌(Ulocladium oudemansii)，特別HRU3菌株(例如Botry-Zen Ltd,NZ之Botry-Zen®)；(B2.84)黑白輪孢菌(Verticillium albo-atrum)(之前V.dahliae)WCS850菌株(CBS 276.92；例如Tree Care Innovations之Dutch Trig)；(B2.86)厚垣輪孢菌(Verticillium chlamydosporium)；(B2.87)棘孢木黴菌ICC 012菌株和蓋姆斯木黴菌ICC 080菌株之混合物(產品為，例如Bayer CropScience LP,US之BIO-TAMTM)。 In some specific examples, the biological control agent is a compound that produces fengycin or plipastatin-type compounds, iturin-type compounds, and / or surfactin-type ) Compounds of Bacillus subtilis or Bacillus amyloliquefaciens strains. For the background, please see the following review article: Ongena, M., et al., " Bacillus Lipopeptides: Versatile Weapons for Plant Disease Biocontrol," Trends in Microbiology, Vol 16, No. 3, March 2008, pp. 115-125. Bacillus strains capable of producing lipopeptides include Bacillus subtilis QST713 (available as SERENADE OPTI or SERENADE ASO from Bayer CropScience LP, US, with NRRL accession number B21661 and described in U.S. Patent No. 6,060,051), and liquefied Bacillus amyloliquefaciens D747 strain (available as Double Nickel ™ from Certis, US with accession number FERM BP-8234 and described in US Patent No. 7,094,592); Bacillus subtilis MBI600 (available as SUBTILEX ® from Becker Underwood, US EPA registration number 71840-8) ; Bacillus subtilis Y1336 (available as BIOBAC ® WP from Bion-Tech, Taiwan, registered as a biofungicide in Taiwan, registration numbers 4764, 5454, 5096, and 5277); liquefied starch Bacillus, especially FZB42 strains (available as RHIZOVITAL ® from ABiTEP, DE); and liquefied starch Bacillus subtilis variants FZB24 (available from Novozymes Biologicals Inc., Salem, Virginia or Syngenta Crop Protection, LLC, Greensboro, North Carolina is a fungicide TAEGRO ® or TAEGRO ® ECO (EPA registration number 70127-5); and (B2) fungi, such as: (B2.1) Pleurotus tenuis ( Co niothyrium minitans ), especially CON / M / 91-8 strains (accession number DSM-9660; for example, Contans® from Bayer); ( B2.2 ) Metschnikowia fructicola strains, especially NRRL Y-30752 strains (E.g. Shemer®); (B2.3) Microsphaeropsis ochracea (e.g. Microx® from Prophyta); (B2.5) Trichoderma spp. Including Trichoderma spp. ( Trichoderma atroviride ), described in the International Patent Application No. PCT / IT2008 / 000196 SC1 strain); (B2.6) Trichoderma harzianum rifai KRL-AG2 strain ( liquidly referred to as T-22 strain, / ATCC 208479, such as PLANETSHIELD T-22G, Rootshield® and TurfShield from BioWorks, US; (B2.14) Gliocladium roseum , 321U strain, from WFStoneman Company LLC; (B2.35) yellow basket Talaromyces flavus , V117b strain; (B2.36) Trichoderma asperellum , ICC 012 strain from Isagro; (B2.37) Trichoderma SKT-1 strain (e.g. ECO-HOPE®, (From Kumiai Chemical Industry); (B2.38) Trichoderma deepum CNCM I-1237 strain (e.g. Esquiv e® WP from Agrauxine, FR); (B2.39) Trichoderma spp. V08 / 002387; (B2.40) Trichoderma spp. NMI V08 / 002388; (B2.41) Trichoderma spp. Strain NMI number V08 / 002389; (B2.42) Trichoderma deep green strain NMI number V08 / 002390; (B2.43) Trichoderma deep strain LC52 (e.g. Tenet from Agrimm Technologies Limited); (B2.44) Deep Trichoderma green strain ATCC 20476 (IMI 206040); (B2.45) Trichoderma dark green strain T11 (IMI352941 / CECT20498); (B2.46) Trichoderma harmatum ; (B2.47) Uncooked wood Molds; (B2.48) Trichoderma harzianum T39 (such as Trichodex® from Makhteshim, US); (B2.49) Trichoderma harzianum, especially KD strains (such as Trichoplus, from Biological Control Products, SA (by Becker (Obtained from Underwood)); (B2.50) Trichoderma harzianum ITEM 908 strain (such as Triumum-P from Koppert); (B2.51) Trichoderma harzianum TH35 strain (such as Root-Pro of Mycontrol); (B2. 52) green Trichoderma (Trichoderma virens) (also referred to as green sticky Scopulariopsis (Gliocladium virens)), in particular GL-21 strain (e.g. of Certis US SoilGard 12G); (B2.53) green Trichoderma (Tric hoderma viride ), TV1 strains (e.g. Trianum-P of Koppert); (B2.54) Ampelomyces quisqualis , especially AQ 10 strains (e.g. AQ 10® of IntrachemBio Italia); (B2.56) short buds B. spp., Especially the spores of DSM14940 strain; (B2.57) S. spores, spores of DSM 14941; (B2.58) S. spores, spores, DSM14940 and DSM 14941 (E.g. Botector® of bio-ferm, CH); (B2.64) Cladosporium cladosporioides , H39 strain (from Stichting Dienst Landbouwkundig Onderzoek); (B2.69) Gliocladium catenulatum ) (synonym: Clonostachys rosea f. catenulate ) J1446 strain (e.g. Prestop® from AgBio Inc. and Primastop® e.g. Kemira Agro Oy); (B2.70) Lecanicillium lecanii ) (formerly known as Verticillium lecanii conidia) strain KV01 (e.g. Vertalec® of Koppert / Arysta); (B2.71) Penicillium vermiculatum ; (B2.72) Pichia anomala WRL-076 strain (NRRL Y-3 0842); (B2.75) Trichoderma SKT-1 strain (FERM P-16510); (B2.76) Trichoderma SKT-2 strain (FERM P-16511); (B2.77) Dark green Trichoderma SKT-3 strain (FERM P-17021); (B2.78) Trichoderma gamsii (formerly T.viride ) ICC080 strain (IMI CC 392151 CABI, such as AGROBIOSOL DE MEXICO, BioDerma of SADE CV ); (B2.79) Trichoderma harzianum DB 103 strain (e.g. T-Gro 7456 from Dagutat Biolab); (B2.80) Trichoderma polysporum IMI 206039 strain (e.g. BINAB Bio-Innovation AB, Sweden) Binab TF WP); (B2.81) Trichoderma stromaticum (such as Ceplac, Tricovab, Brazil); (B2.83) Ulocladium oudemansii , especially HRU3 strain ( (For example, Botry-Zen® of Botry-Zen Ltd, NZ); (B2.84) Verticillium albo-atrum (formerly V. dahliae ) WCS850 strain (CBS 276.92; for example, Dutch Trig by Tree Care Innovations); (B2.86) Verticillium chlamydosporium ; (B2.87) a mixture of Trichoderma ICC 012 strain and Trichoderma ICC 080 strain (product is, for example, Bayer Crop Science LP, US BIO-TAM ™ ).

可與本發明化合物和組成物組合的生物防治劑之其他的實例有：由下列組成之群中選出的細菌：枯草芽孢桿菌，特別是枯草芽孢桿菌CNCM I-1562菌株和堅强芽孢桿菌(Bacillus firmus)I-1582菌株(登錄號CNCM I-1582)，枯草芽孢桿菌OST 30002(登錄號NRRL B-50421)，蘇雲金芽孢桿菌(Bacillus thuringiensis)，特別是蘇雲金芽孢桿菌以色列亞種(israelensis)(血清型H-14)，AM65-52菌種(登錄號ATCC 1276)，蘇雲金芽孢桿菌鮎澤亞種(B.thuringiensis subsp.aizawai)，特別是ABTS-1857菌株(SD-1372)，蘇雲金芽孢桿菌庫斯塔基亞種(B.thuringiensis subsp.kurstaki)HD-1菌株，蘇雲金芽孢桿菌擬步行蟲亞種(B.thuringiensis subsp.tenebrionis)NB 176菌株(SD-5428)，穿刺巴斯德芽菌(Pasteuria penetrans)，巴斯德芽菌(Pasteuria spp.)(腎行線蟲(Rotylenchulus reniformis))-PR3(登錄號ATCC SD-5834)，細黃鏈黴菌(Streptomyces microflavus)AQ6121菌株(=QRD 31.013,NRRL B-50550)及鮮黃鏈黴菌(Streptomyces galbus)AQ 6047(登錄號NRRL 30232)；由下列組成之群中選出的真菌和酵母菌：球孢白僵菌(Beauveria bassiana)，特別是ATCC 74040菌株，蠟蚧輪枝菌(Lecanicillium spp.)，特別是HRO LEC 12菌株，黑殭菌(Metarhizium anisopliae)，特別是菌株F52(DSM3884或ATCC 90448)，玫煙色擬青黴菌(Paecilomyces fumosoroseus)(目前：玫烟色棒束孢菌(Isaria fumosorosea)，特別是IFPC 200613菌株或Apopka 97菌株(登錄號ATCC 20874)和淡紫擬青黴菌(Paecilomyces lilacinus)，特別是淡紫擬青黴菌(P.lilacinus)251菌株(AGAL 89/030550)；由下列組成之群中選出的病毒：茶姬捲葉蛾(Adoxophyes orana)(夏果捲葉蟲)顆粒病病毒(GV)、蘋果蠹蛾(Cydia pomonella)(內蠹蛾)顆粒病病毒(GV)、棉鈴實夜蛾(Helicoverpa armigera)(棉蛉蟲)核多角體病毒(NPV)、甜菜夜蛾(Spodoptera exigua)mNPV、草地夜蛾(Spodoptera frugiperda)(秋行軍蟲)mNPV和斜紋夜蛾(Spodoptera littoralis)(非洲棉葉蟲)NPV。 Examples with other biocontrol agents of the compounds and compositions of the present invention has the composition: selected from the group consisting of bacteria: Bacillus subtilis, especially Bacillus subtilis strain CNCM I-1562 and Bacillus firmus (Bacillus firmus ) strain I-1582 (accession number CNCM I-1582), Bacillus subtilis OST 30002 (accession number NRRL B-50421), Bacillus thuringiensis , especially Israeli subspecies of israelensis (serum Type H-14), AM65-52 strain (accession number ATCC 1276), B. thuringiensis subsp. Aizawai , especially ABTS-1857 strain (SD-1372), B. thuringiensis B. thuringiensis subsp. Kurstaki HD-1 strain, B. thuringiensis subsp. Tenenebrionis NB 176 strain (SD-5428), and Pasteuria puncture penetrans ), Pasteuria spp. (Rotylenchulus reniformis) -PR3 (accession number ATCC SD-5834), Streptomyces microflavus AQ6121 strain (= QRD 31.013, NRRL B -50,550) and Streptomyces galbus (Streptomyces galbus) AQ 6047 (Accession No. NRRL 30232); selected from the group consisting of yeasts and fungi: Beauveria (Beauveria bassiana), in particular strain ATCC 74040, Lecanicillium spp. , Especially HRO LEC 12 strain, Metarhizium anisopliae , especially strain F52 (DSM3884 or ATCC 90448), Paecilomyces fumosoroseus (currently: Isaria fumosorosea , especially IFPC 200613 strain or Apopka 97 strain (accession number ATCC 20874) and Paecilomyces lilacinus , especially P. lilacinus Strain 251 (AGAL 89/030550); virus selected from the group consisting of: Adoxophyes orana (leaf leaf roller ), Granulovirus (GV), Cydia pomonella (internal pupa ) Moth) Granulosis virus (GV), Helicoverpa armigera (cotton borer) nuclear polyhedrosis virus (NPV), Spodoptera exigua mNPV, Spodoptera frugiperda (Autumn parasite) mNPV and twill Moth (Spodoptera littoralis) (African cotton leaf worm) NPV.

細菌和真菌可加到植物或植物部位或植物器官中作為「接種劑」，利用其特定的性質，提升植物生長和植物健康。實例有：土壤桿菌屬(Agrobacterium spp.)、莖瘤固氮根瘤菌(Azorhizobium caulinodans)、固氮螺菌屬(Azospirillum spp.)、固氮菌屬(Azotobacter spp.)、慢生根瘤菌屬(Bradyrhizobium spp.)、伯克霍爾德氏菌屬(Burkholderia spp.)，特別是洋蔥伯克霍爾德菌(Burkholderia cepacia)(以前稱為洋蔥假單胞菌(Pseudomonas cepacia))、巨孢囊黴屬(Gigaspora spp.)或單孢巨孢囊黴(Gigaspora monosporum)、球囊黴屬(Glomus spp.)、蠟蘑屬(Laccaria spp.)、布氏乳桿菌(Lactobacillus buchneri)、類球囊黴屬(Paraglomus spp.)、豆包菌(Pisolithus tinctorus)、假單胞菌屬(Pseudomonas spp.)、根瘤菌屬(Rhizobium spp.)，特別是三葉草根瘤菌(Rhizobium trifolii)、須腹菌屬(Rhizopogon spp.)、硬皮鏽菌 屬(Scleroderma spp.)、乳牛肝菌屬(Suillus spp.)和鏈黴菌屬(Streptomyces spp.)。 Bacteria and fungi can be added to plants or plant parts or plant organs as "inoculants", using their specific properties to enhance plant growth and plant health. Examples are: Agrobacterium spp. , Azorhizobium caulinodans , Azospirillum spp. , Azotobacter spp. , Bradyrhizobium spp. ), Burkholderia spp. , Especially Burkholderia cepacia (formerly known as Pseudomonas cepacia ), Macrocystis ( Gigaspora spp. ) Or Gigaspora monosporum , Glomus spp. , Laccaria spp. , Lactobacillus buchneri , Glomus-like Paraglomus spp. ), Pisolithus tinctorus , Pseudomonas spp. , Rhizobium spp. , Especially Rhizobium trifolii , Rhizopogon spp. ), Scleroderma spp. , Suillus spp. , And Streptomyces spp .

植物萃取物和由微生物形成的產品(包括蛋白和二級代謝物)，其可用作生物防治劑，例如：大蒜(Allium sativum)、苦艾(Artemisia absinthium)、印楝素(azadirachtin)、Biokeeper WP、Cassia nigricans、苦皮藤(Celastrus angulatus)、土荊芥(Chenopodium anthelminticum)、甲殼素(chitin)、Armour-Zen、鱗毛蕨(Dryopteris filix-mas)、問荊(Equisetum arvense)、Fortune Aza、Fungastop、Heads Up(奎奴亞藜(Chenopodium quinoa)皂苷提取物)、除蟲菊(Pyrethrum)/除蟲菊酯類(Pyrethrins)、蘇里南苦木(Quassia amara)、櫟樹屬(Quercus)、皂樹屬(Quillaja)、Regalia、「RequiemTM Insecticide」、魚藤酮(rotenone)、魚尼丁(ryania)/蘭尼鹼(ryanodine)、聚合草(Symphytum officinale)、艾菊(Tanacetum vulgare)、麝香草酚(thymol)、Triact 70、TriCon、旱金蓮(Tropaeulum majus)、大蕁麻(Urtica dioica)、Veratrin、槲寄生(Viscum album)、十字花科(Brassicaceae)萃取物，特別是油菜粉或芥末粉。 Plant extracts and products (including proteins and secondary metabolites) formed by microorganisms, which can be used as biological control agents, such as: garlic ( Allium sativum ), absinthe ( Artemisia absinthium ), azadirachtin, Biokeeper WP, Cassia nigricans , Celastrus angulatus , Chenopodium anthelminticum , chitin, Armour-Zen, Dryopteris filix-mas , Equisetum arvense , Fortune Aza, Fungastop, Heads Up (quinoa (Chenopodium quinoa) saponin extract), pyrethrum (pyrethrum) / pyrethrins (pyrethrins), Surinam quassia (quassia amara), the genus oak (Quercus), soap Quillaja , Regalia, "Requiem TM Insecticide", rotenone, ryania / ryanodine, Symphytum officinale , Tanacetum vulgare , thymol (thymol), Triact 70, TriCon, Tropaeulum majus , Urtica dioica , Veratrin, Mistletoe ( Viscum album ), Brassicaceae extract, special It is canola or mustard.

可與本發明化合物和組成物混合的個別殺昆蟲劑、殺蟎劑和殺線蟲劑之實例有： Examples of individual insecticides, acaricides and nematicides that can be mixed with the compounds and compositions of the present invention are:

(1)乙醯膽鹼酯酶(AChE)抑制劑，例如胺甲酸酯類，例如阿納寧(alanycarb)、得滅克(aldicarb)、免敵克(bendiocarb)、免扶克(benfuracarb)、佈嘉信(butocarboxim)、佈斯嘉信(butoxycarboxim)、加保利(carbaryl)、加保扶(carbofuran)、丁基加保扶(carbosulfan)、愛殺芬卡(ethiofencarb)、丁基滅必蝨(fenobucarb)、覆滅蟎(formetanate)、呋線威(furathiocarb)、滅必蝨(isoprocarb)、滅賜克(methiocarb)、納乃得(methomyl)、治滅蝨(metolcarb)、歐殺滅(oxamyl)、抗蚜威(pirimicarb)、殘殺威(propoxur)、硫雙威(thiodicarb)、久效威(thiofanox)、唑蚜威(triazamate)、混滅威(trimethacarb)、XMC及滅殺威(xylylcarb)；或有機磷酸酯類，例如歐殺松(acephate)、甲基吡啶磷(azamethiphos)、益棉磷(azinphos-ethyl)、穀速松(azinphos-methyl)、硫線磷(cadusafos)、氯氧磷(chlorethoxyfos)、毒蟲畏(chlorfenvinphos)、氯甲硫磷(chlormephos)、甲基陶斯松(chlorpyrifos-methyl)、蠅毒磷(coumaphos)、殺螟 腈(cyanophos)、滅賜松(demeton-S-methyl)、大利松(diazinon)、敵敵畏(dichlorvos)/DDVP、百治磷(dicrotophos)、大滅松(dimethoate)、二甲基毒蟲畏(dimethylvinphos)、乙拌磷(disulfoton)、EPN、乙硫磷(ethion)、滅線磷(ethoprophos)、伐滅磷(famphur)、苯線磷(fenamiphos)、殺螟硫磷(fenitrothion)、倍硫磷(fenthion)、噻唑膦(fosthiazate)、飛達松(heptenophos)、依米塞扶(imicyafos)、異柳磷(isofenphos)、異丙基O-(甲氧基胺基硫基磷醯基)水楊酸酯、異

Figure TW201945344A_D0140
唑磷(isoxathion)、馬拉硫磷(malathion)、滅蚜磷(mecarbam)、甲胺磷(methamidophos)、殺撲磷(methidathion)、速滅磷(mevinphos)、久效磷(monocrotophos)、二溴磷(naled)、氧樂果(omethoate)、亞碸磷(oxydemeton-methyl)、甲基對硫磷(parathion-methyl)、稻豐散(phenthoate)、甲拌磷(phorate)、伏殺硫磷(phosalone)、亞胺硫磷(phosmet)、磷胺(phosphamidon)、肟硫磷(phoxim)、甲基嘧啶磷(pirimiphos-methyl)、丙溴磷(profenofos)、胺丙畏(propetamphos)、丙硫磷(prothiofos)、白克松(pyraclofos)、必芬松(pyridaphenthion)、拜裕松(quinalphos)、治螟磷(sulfotep)、丁基嘧啶磷(tebupirimfos)、亞培松(temephos)、託福松(terbufos)、殺蟲畏(tetrachlorvinphos)、硫滅松(thiometon)、三唑磷(triazophos)、三氯松(trichlorfon)及繁米松(vamidothion)。 (1) Acetylcholinesterase (AChE) inhibitors, such as carbamates, such as ananycarb, aldicarb, bendiocarb, benfuracarb, cloth Butoscarboxim, butoxycarboxim, carbaryl, carbofuran, carbosulfan, ethiofencarb, fenobucarb , Formetanate, furathiocarb, isoprocarb, metiocarb, methodyl, metolcarb, oxamyl, anti- Pirimicarb, propoxur, thiodicarb, thiofanox, triazamate, trimethacarb, XMC and xylylcarb; or Organophosphates, such as acephate, azamethiphos, azinphos-ethyl, azonphos-methyl, cadusafos, oxychloride ( chlorethoxyfos), chlorfenvinphos, chlormephos, chlorpyrifos-methyl, coumaphos , Cyanophos, demeton-S-methyl, diazinon, dichlorvos / DDVP, dicrotophos, dimethoate, dimethyl poison Dimethylvinphos, disulfoton, EPN, ethion, ethoprophos, famphur, fenamiphos, fenitrothion , Fenthion, fosthiazate, heptenophos, imicyafos, isofenphos, isopropyl O- (methoxyaminothiothiophosphine) Fluorenyl) salicylate
Figure TW201945344A_D0140
Isoxathion, malathion, mecarbam, metamidophos, methidathion, mevinphos, monocrotophos, two Brominated (naled), omethoate, oxydemeton-methyl, parathion-methyl, rice phenthoate, phorate, phorfos Phosphorus (phosalone), phosmet (phosmet), phosphamidon, phoxim, pirimiphos-methyl, profenofos, propetamphos, Prothiofos, pyraclofos, pyridaphenthion, quinalphos, sulfotep, tebupirimfos, temephos, tofosone (terbufos), tetrachlorvinphos, thiometon, triazophos, trichlorfon, and vamidomion.

(2)GABA-閘控氯離子通道阻斷劑，例如環雙烯-有機氯類，例如可氯丹(chlordane)和安殺番(endosulfan)或苯基吡唑(菲普魯來斯(fiproles))，例如益斯普(ethiprole)和芬普尼(fipronil)。 (2) GABA-gated chloride ion channel blockers, such as cyclodiene-organochlorines, such as chlordane and endosulfan or phenylpyrazole (fiproles )), Such as ethiprole and fipronil.

(3)鈉通道調節劑，例如擬除蟲菊酯(pyrethroid)，例如氟丙菊酯(acrinathrin)、烯丙菊酯(allethrin)、d-順-反烯丙菊酯，d-反烯丙菊酯、畢芬寧(bifenthrin)、百亞列寧(bioallethrin)、百亞列寧-S-環戊烯基異構物、生物苄呋菊酯(bioresmethrin)、乙氰菊酯(cycloprothrin)、賽扶寧(cyfluthrin)、β-賽扶寧、賽洛寧(cyhalothrin)、λ-賽洛寧、γ-賽洛寧、賽滅寧(cypermethrin)、α-賽滅寧、β-賽滅寧、θ-賽滅寧、ζ-賽滅寧、賽酚寧(cyphenothrin)[(1R)-反式異構物]、第滅寧(deltamethrin)、益避寧(empenthrin)[(EZ)-(1R)異構物]、益化利(esfenvalerate)、依芬寧(etofenprox)、芬普寧(fenpropathrin)、芬化利 (fenvalerate)、護賽寧(flucythrinate)、氟氯苯氰菊酯(flumethrin)、福化利(tau-fluvalinate)、合芬寧(halfenprox)、依普寧(imiprothrin)、克特寧(kadethrin)、momfluorothrin、百滅寧(permethrin)、苯醚菊酯(phenothrin)[(1R)-反式異構物]、炔丙菊酯(prallethrin)、除蟲菊素(pyrethrins)(除蟲菊pyrethrum)、苄呋菊酯(resmethrin)、矽護芬(silafluofen)、七氟菊酯(tefluthrin)、胺菊酯(tetramethrin)、胺菊酯[(1R)-異構物]、四溴菊酯(tralomethrin)及四氟苯菊酯(transfluthrin)或DDT或甲氧氯(methoxychlor)。 (3) Sodium channel regulators, such as pyrethroids, such as acrithrin, allethrin, d-cis-transallethrin, d-transallyl Permethrin, bifenthrin, bioallethrin, bailenin-S-cyclopentenyl isomers, bioresmethrin, cycloprothrin, cyprothrin (bifenthrin) cyfluthrin), β-Syfronin, cyhalothrin, λ-Syronin, γ-Syronin, cypermethrin, α-Syphenin, β-Syphenin, θ-Sy Metronid, ζ-cyphenidin, cyphenothrin [(1R) -trans isomer], deltamethrin, empenthrin [(EZ)-(1R) isomer Properties), esfenvalerate, etofenprox, fenpropathrin, fenvalerate, flucythrinate, flumethrin, fluvalin (tau-fluvalinate), halfenprox, imiprothrin, kadethrin, momfluorothrin, permethrin, phenothrin ((1R) -trans-isomer Structure], prallethrin , Pyrethrins (pyrethrum), resmethrin, silafluofen, tefluthrin, tetramethrin, pyrethrin [( 1R) -isomer], tralomethrin and transfluthrin or DDT or methoxychlor.

(4)尼古丁乙醯膽鹼受體(nAChR)競爭性調節劑，例如新菸鹼類，例如亞滅培(acetamiprid)、可尼丁(clothianidin)、達特南(dinotefuran)、益達胺(imidacloprid)、烯啶蟲胺(nitenpyram)、噻蟲啉(thiacloprid)和噻蟲

Figure TW201945344A_D0141
(thiamethoxam)或菸鹼或氟啶蟲胺腈(sulfoxaflor)或氟吡呋喃酮(flupyradifurone)。 (4) Competitive modulators of nicotine acetylcholine receptor (nAChR), such as neonicotinoids, such as acetamiprid, clothianidin, dinotefuran, and Idamin ( imidacloprid), nitenpyram, thiacloprid, and thiacloprid
Figure TW201945344A_D0141
(thiamethoxam) or nicotine or sulfoxaflor or flupyradifurone.

(5)尼古丁乙醯膽鹼受體(nAChR)之變構調節劑，例如多殺菌素(spinosyn)，例如賜拓侖(spinetoram)和賜諾殺(spinosad)。 (5) Allosteric modulators of nicotine acetocholine receptor (nAChR), such as spinosyn, such as spinortoram and spinosad.

(6)麩胺酸-閘控氯離子通道(GluCl)變構調節劑，例如，阿維菌素(avermectin)/米貝菌素(milbemycin)，例如阿巴汀(abamectin)、因滅汀苯甲酸鹽(emamectin benzoate)、雷匹美汀(lepimectin)和密滅汀(milbemectin)。 (6) Glutamate-gated chloride ion channel (GluCl) allosteric modulators, for example, avermectin / milbemycin, such as abatectin, indipylbenzene Formate (emamectin benzoate), lepimectin and milbemectin.

(7)保幼激素模擬物，例如保幼激素類似物，例如烯蟲乙酯(hydroprene)、烯蟲炔酯(kinoprene)和美賜年(methoprene)或苯氧威(fenoxycarb)或蚊蟎醚(pyriproxyfen)。 (7) Juvenile hormone mimics, such as juvenile hormone analogs, such as hydroprene, kinoprene, and metoprene or fenoxycarb or fenoxycarb ( pyriproxyfen).

(8)混雜非特定(多位點)抑制劑，例如烷基鹵化物，例如甲基溴和其他烷基鹵化物；或氯化苦(Chloropicrin)或硫醯氟(sulfuryl fluoride)或硼砂(borax)或吐酒石(tartar emetic)或異氰酸甲酯生成劑，例如邁隆(dazomet)和斯美地(metam)。 (8) Miscellaneous non-specific (multi-site) inhibitors, such as alkyl halides, such as methyl bromide and other alkyl halides; or Chloropicrin, sulfuryl fluoride, or borax ) Or tartar emetic or methyl isocyanate generators such as dazomet and metam.

(9)弦音感覺器官調節劑，例如派滅淨(pymetrozine)或氟尼胺(flonicamid)。 (9) String tone sensory organ modulating agents, such as pymetrozine or flonicamid.

(10)蟎生長抑制劑，例如克芬蟎(clofentezine)、合賽多(hexythiazox)和敵氟淨(diflovidazin)或乙蟎唑(etoxazole)。 (10) Mite growth inhibitors, such as clofentezine, hexythiazox, and diflovidazin, or etoxazole.

(11)昆蟲腸道膜之微生物干擾劑，例如蘇雲金芽孢桿菌以色列亞種、球形芽抱桿菌紡錘變種(Bacillus sphaericus)、蘇雲金芽孢桿菌鮎澤亞種、蘇雲金芽孢桿菌庫斯塔基亞種、蘇雲金芽孢桿菌擬步行蟲亞種，及B.t.植物蛋白：Cry1Ab、Cry1Ac、Cry1Fa、Cry1A.105、Cry2Ab、Vip3A、mCry3A、Cry3Ab、Cry3Bb、Cry34Ab1/35Ab1。 (11) Microbial interfering agents for insect intestinal membranes, such as Bacillus thuringiensis subspecies Israel, Bacillus sphaericus , Bacillus thuringiensis subspecies, Bacillus thuringiensis Kustaki subspecies, Bacillus thuringiensis Bacteria parasites, and Bt plant proteins: Cry1Ab, Cry1Ac, Cry1Fa, Cry1A.105, Cry2Ab, Vip3A, mCry3A, Cry3Ab, Cry3Bb, Cry34Ab1 / 35Ab1.

(12)粒線體ATP合成酶之抑制劑，例如ATP干擾劑，例如汰芬隆(diafenthiuron)或有機錫化合物，例如亞環錫(azocyclotin)、錫蟎丹(cyhexatin)及芬布賜(fenbutatin oxide)或毆蟎多(Propargite)或得脫蟎(Tetradifon)。 (12) Inhibitors of mitochondrial ATP synthase, such as ATP interfering agents, such as diafenthiuron or organotin compounds, such as azocyclotin, cyhexatin, and fenbutatin oxide) or Propargite or Tetradifon.

(13)經由擾亂質子梯度作用之氧化磷酸化去偶合劑，例如蟲蟎腈(chlorfenapyr)、DNOC和沙氟米得(sulfluramid)。 (13) Oxidative phosphorylation decoupling agents, such as chlorfenapyr, DNOC, and sulfluramid, that disturb proton gradients.

(14)尼古丁乙醯膽鹼受體通道阻斷劑，例如免速達(bensultap)、培丹鹽酸鹽(cartap hydrochloride)、硫賜安(thiocyclam)和殺蟲單(thiosultap-sodium)。 (14) Nicotine acetylcholine receptor channel blockers, such as bensultap, cartap hydrochloride, thiocyclam, and thiosultap-sodium.

(15)甲殼素生物合成抑制劑，第0型，例如雙三氟蟲脲(bistrifluron)、克福隆(chlofluazuron)、二福隆(diflubenzuron)、氟環脲(flucycloxuron)、氟芬隆(flufenoxuron)、六伏隆(hexaflumuron)、祿芬隆(lufenuron)、諾瓦隆(novaluron)、紐伏隆(noviflumuron)、得福隆(teflubenzuron)及殺蟲隆(triflumuron)。 (15) Chitin biosynthesis inhibitor, type 0, such as bistrifluron, chlofluazuron, diflubenzuron, flucycloxuron, flufenoxuron ), Hexaflumuron, lufenuron, novaluron, noviflumuron, teflubenzuron, and triflumuron.

(16)甲殼素生物合成抑制劑，第1型，例如布芬淨(buprofezin)。 (16) Chitin biosynthesis inhibitor, type 1, such as bufofezin.

(17)蛻皮干擾劑(特別是雙翅目)，例如賽滅淨(Cyromazine)。 (17) Molting interferences (especially Diptera), such as Cyromazine.

(18)蛻皮素受體促效劑，例如環蟲醯肼(chromafenozide)、氯蟲醯肼(halofenozide)、甲氧蟲醯肼(methoxyfenozide)及蟲醯肼(tebufenozide)。 (18) ecdysone receptor agonists, such as chromafenozide, halofenozide, methoxyfenozide, and tebufenozide.

(19)奧克巴胺(octopamine)受體促效劑，例如三亞蟎(amitraz)。 (19) Octopamine receptor agonists, such as amitraz.

(20)粒線體複合物III電子傳遞抑制劑，例如伏蟻腙(hydramethylnon)或亞醌蟎(acequinocyl)或嘧蟎酯(fluacrypyrim)。 (20) Mitochondrial complex III electron transfer inhibitors, such as hydramethylnon or acequinocyl or fluacrypyrim.

(21)粒線體複合物I電子傳遞抑制劑，例如來自METI殺蟎劑之群，例如喹蟎醚(fenazaquin)、芬普蟎(fenpyroximate)、畢汰芬(pyrimidifen)、噠蟎靈(pyridaben)、吡蟎胺(tebufenpyrad)和唑蟲醯胺(tolfenpyrad)或魚藤酮(rotenone)(Derris)。 (21) Mitochondrial complex I electron transfer inhibitors, for example from the group of METI acaricides, such as fenazaquin, fenpyroximate, pyrimidifen, pyridaben ), Tebufenpyrad and tolfenpyrad or rotenone (Derris).

(22)電壓-依賴的鈉通道阻斷劑，例如茚蟲威(indoxacarb)或美氟腙(metaflumizon)。 (22) Voltage-dependent sodium channel blockers, such as indoxacarb or metaflumizon.

(23)乙醯基-CoA羧基酶之抑制劑，例如特窗酸(tetronic acid)和特拉姆酸(tetramic acid)衍生物，例如螺蟎酯(spirodiclofen)、螺甲蟎酯(spiromesifen)及螺泰曲美(spirotetramate)。 (23) Inhibitors of acetamyl-CoA carboxylase, such as tetronic acid and tetramic acid derivatives, such as spirodiclofen, spiromesifen, and Spirotetramate.

(24)粒線體複合物IV電子傳遞抑制劑，例如膦類，例如磷化鋁、磷化鈣，膦和磷化鋅或氰化物、氰化鈣、氰化鉀和氰化鈉。 (24) Mitochondrial complex IV electron transfer inhibitors such as phosphines such as aluminum phosphide, calcium phosphide, phosphine and zinc phosphide or cyanide, calcium cyanide, potassium cyanide and sodium cyanide.

(25)粒線體複合物II電子傳遞抑制劑，例如β-酮腈衍生物，例如賽諾吩(cyenopyrafen)和賽芬蟎(Cyflumetofen)，和甲醯苯胺類，例如pyflubumide。 (25) Mitochondrial complex II electron transport inhibitors, such as β-ketonitrile derivatives, such as cyenopyrafen and Cyflumetofen, and toluidine, such as pyflubumide.

(28)雷若丁(Ryanodine)受體調節劑，例如二醯胺類，例如剋安勃(chlorantraniliprole)、氰蟲醯胺(Cyantraniliprole)和氟蟲醯胺(flubendiamide)， (28) Ryanodine receptor modulators, such as diamines, such as chlorantraniliprole, Cyantraniliprole, and flubendiamide,

另外的活性成份，例如雙丙環蟲酯(Afidopyropen)、阿弗索拉納(Afoxolaner)、印楝素(Azadirachtin)、苯克噻(Benclothiaz)、苯蟎特(Benzoximate)、聯苯肼酯(Bifenazate)、溴蟲氟苯雙醯胺(Broflanilide)、溴蟎酯(Bromopropylate)、滅蟎猛(Chinomethionat)、右旋反式氯丙炔菊酯(Chloroprallethrin)、冰晶石(Cryolite)、環溴蟲醯胺(Cyclaniliprole)、環氧蟲啶(Cycloxaprid)、氯氟氰蟲醯胺(Cyhalodiamide)、Dicloromezotiaz、大克蟎(Dicofol)、E-甲氧苄氟菊酯(Epsilon Metofluthrin)、E-甲氧苄氟菊酯單體、Flometoquin、三氟咪啶醯胺(Fluazaindolizine)、氟噻蟲碸(Fluensulfone)、嘧蟲胺(Flufenerim)、氟菌蟎酯(Flufenoxystrobin)、丁蟲臆(Flufiprole)、Fluhexafon、氟批菌醯胺(Fluopyram)、氟雷拉納(Fluralaner)、Fluxametamide、呋喃蟲醯肼(Fufenozide)、戊吡蟲胍(Guadipyr)、氯氟醚菊酯(Heptafluthrin)、氯噻啉(Imidaclothiz)、依普同(Iprodione)、K-畢芬寧(Kappa-Bifenthrin)、K-七氟菊酯(Kappa-Tefluthrin)、Lotilaner、氟醚菊酯(Meperfluthrin)、呱蟲啶(Paichongding)、三氟甲吡醚(Pyridalyl)、Pyrifluquinazon、嘧螨胺(Pyriminostrobin)、賜派芬(Spirobudiclofen)、四氟醚菊酯(Tetramethylfluthrin)、Tetraniliprole、剋安勃(Tetrachlorantraniliprole)、Tigolaner、Tioxazafen、硫氟肟醚(Thiofluoximate)、三氟苯嘧啶(Triflumezopyrim)和碘甲烷 (Methyliodide)；此外以堅強芽胞桿菌為基礎的製備物(I-1582、BioNeem、Votivo)，及下列化合物：1-{2-氟-4-甲基-5-[(2,2,2-三氟乙基)亞磺醯基]苯基}-3-(三氟甲基)-1H-1,2,4-三唑-5-胺(得自WO2006/043635)(CAS 885026-50-6)、{1'-[(2E)-3-(4-氯苯基)丙-2-烯-1-基]-5-氟螺[吲哚-3,4'-哌啶]-1(2H)-基}(2-氯吡啶-4-基)甲酮(得自WO2003/106457)(CAS 637360-23-7)、2-氯-N-[2-{1-[(2E)-3-(4-氯苯基)丙-2-烯-1-基]哌啶-4-基}-4-(三氟甲基)苯基]異菸鹼醯胺(得自WO2006/003494)(CAS 872999-66-1)、3-(4-氯-2,6-二甲基苯基)-4-羥基-8-甲氧基-1,8-二氮螺[4.5]癸-3-烯-2-酮(得自WO 2010052161)(CAS 1225292-17-0)、3-(4-氯-2,6-二甲基苯基)-8-甲氧基-2-側氧-1,8-二氮螺[4.5]癸-3-烯-4-基乙基碳酸酯(得自EP 2647626)(CAS-1440516-42-6)、4-(丁-2-炔-1-基氧基)-6-(3,5-二甲基哌啶-1-基)-5-氟嘧啶(得自WO2004/099160)(CAS 792914-58-0)、PF1364(得自JP2010/018586)(CAS 1204776-60-2)、N-[(2E)-1-[(6-氯吡啶-3-基)甲基]吡啶-2(1H)-亞基]-2,2,2-三氟乙醯胺(得自WO2012/029672)(CAS 1363400-41-2)、(3E)-3-[1-[(6-氯-3-吡啶基)甲基]-2-亞吡啶基]-1,1,1-三氟-丙-2-酮(得自WO2013/144213)(CAS 1461743-15-6)、N-[3-(苯甲基胺甲醯基)-4-氯苯基]-1-甲基-3-(五氟乙基)-4-(三氟甲基)-1H-吡唑-5-甲醯胺(得自WO2010/051926)(CAS 1226889-14-0)、5-溴-4-氯-N-[4-氯-2-甲基-6-(甲基胺甲醯基)苯基]-2-(3-氯-2-吡啶基)吡唑-3-甲醯胺(得自CN103232431)(CAS 1449220-44-3)、4-[5-(3,5-二氯苯基)-4,5-二氫-5-(三氟甲基)-3-異

Figure TW201945344A_D0142
唑基]-2-甲基-N-(順-1-氧化-3-噻呾基)苯甲醯胺、4-[5-(3,5-二氯苯基)-4,5-二氫-5-(三氟甲基)-3-異
Figure TW201945344A_D0143
唑基]-2-甲基-N-(反-1-氧化-3-噻呾基)苯甲醯胺及4-[(5S)-5-(3,5-二氯苯基)-4,5-二氫-5-(三氟甲基)-3-異
Figure TW201945344A_D0144
唑基]-2-甲基-N-(順-1-氧化-3-噻呾基)苯甲醯胺(得自WO 2013/050317 A1)(CAS 1332628-83-7)、N-[3-氯-1-(3-吡啶基)-1H-吡唑-4-基]-N-乙基-3-[(3,3,3-三氟丙基)亞磺醯基]丙醯胺、(+)-N-[3-氯-1-(3-吡啶基)-1H-吡唑-4-基]-N-乙基-3-[(3,3,3-三氟丙基)亞磺醯基]丙醯胺及(-)-N-[3-氯-1-(3-吡啶基)-1H-吡唑-4-基]-N-乙基-3-[(3,3,3-三氟丙基)亞磺醯基]丙醯胺(得自WO 2013/162715 A2、WO 2013/162716 A2、US 2014/0213448 A1)(CAS 1477923-37-7)、5-[[(2E)-3-氯-2-丙烯-1-基]胺基]-1-[2,6-二氯-4-(三氟甲基)苯基]-4-[(三氟甲基)亞磺醯基]-1H-吡唑-3-甲腈(得自CN 101337937 A)(CAS 1105672-77-2)、3-溴-N-[4-氯-2-甲基-6-[(甲基胺基)硫基甲基]苯基]-1-(3-氯-2-吡啶基)-1H-吡唑-5-甲醯胺、(Liudaibenjiaxuanan，得自CN 103109816 A)(CAS 1232543-85-9)；N-[4-氯-2-[[(1,1-二甲基乙基)胺基]羰基]-6-甲基苯基]-1-(3-氯-2-吡啶基)-3-(氟甲氧基)-1H-吡唑-5-甲醯胺(得自WO 2012/034403 A1)(CAS 1268277-22-0)、N-[2-(5-胺基-1,3,4-噻二唑-2-基)-4-氯-6-甲基苯基]-3-溴-1-(3-氯-2-吡啶基)-1H-吡唑-5-甲醯胺(得自WO 2011/085575 A1)(CAS 1233882-22-8)、4-[3-[2,6-二氯-4-[(3,3-二氯-2-丙烯-1-基)氧基]苯氧基]丙氧基]-2-甲氧基-6-(三氟甲基)嘧啶(得自CN 101337940 A)(CAS 1108184-52-6)；(2E)-及2(Z)-2-[2-(4-氰基苯基)-1-[3-(三氟甲基)苯基]亞乙基]-N-[4-(二氟甲氧基)苯基]肼基甲醯胺(得自CN 101715774 A)(CAS 1232543-85-9)；3-(2,2-二氯乙烯基)-2,2-二甲基-4-(1H-苯并咪唑-2-基)苯基環丙羧酸酯(得自CN 103524422 A)(CAS 1542271-46-4)；(4aS)-7-氯-2,5-二氫-2-[[(甲氧基羰基)[4-[(三氟甲基)硫基]苯基]胺基]羰基]茚并[1,2-e][1,3,4]
Figure TW201945344A_D0145
二
Figure TW201945344A_D0146
-4a(3H)-羧酸甲酯(得自CN 102391261 A)(CAS 1370358-69-2)；6-去氧-3-O-乙基-2,4-二-O-甲基-1-[N-[4-[1-[4-(1,1,2,2,2-五氟乙氧基)苯基]-1H-1,2,4-三唑-3-基]苯基]胺甲酸]-α-L-吡喃甘露糖(得自US 2014/0275503 A1)(CAS 1181213-14-8)；8-(2-環丙基甲氧基-4-三氟甲基-苯氧基)-3-(6-三氟甲基嗒
Figure TW201945344A_D0147
-3-基)-3-氮雜雙環[3.2.1]辛烷(CAS 1253850-56-4)、(8-逆)-8-(2-環丙基甲氧基-4-三氟甲基苯氧基)-3-(6-三氟甲基嗒
Figure TW201945344A_D0148
-3-基)-3-氮雜雙環[3.2.1]辛烷(CAS 933798-27-7)、(8-同)-8-(2-環丙基甲氧基-4-三氟甲基苯氧基)-3-(6-三氟甲基嗒
Figure TW201945344A_D0149
-3-基)-3-氮雜雙環[3.2.1]辛烷(得自WO 2007040280 A1、WO 2007040282 A1)(CAS 934001-66-8)、N-[3-氯-1-(3-吡啶基)-1H-吡唑-4-基]-N-乙基-3-[(3,3,3-三氟丙基)硫基]-丙醯胺(得自WO 2015/058021 A1,WO 2015/058028 A1)(CAS 1477919-27-9)和N-[4-(胺基硫基甲基)-2-甲基-6-[(甲基胺基)羰基]苯基]-3-溴-1-(3-氯-2-吡啶基)-1H-吡唑-5-甲醯胺(得自CN 103265527 A)(CAS 1452877-50-7)、5-(1,3-二氧六圜基-2-基)-4-[[4-(三氟甲基) 苯基]甲氧基]-嘧啶(得自WO 2013/115391 A1)(CAS 1449021-97-9)、3-(4-氯-2,6-二甲基苯基)-4-羥基-8-甲氧基-1-甲基-1,8-二氮雜螺環[4.5]癸-3-烯-2-酮(得自WO 2010/066780 A1,WO 2011/151146 A1)(CAS 1229023-34-0)、3-(4-氯-2,6-二甲基苯基)-8-甲氧基-1-甲基-1,8-二氮雜螺環[4.5]癸-2,4-二酮(得自WO 2014/187846 A1)(CAS 1638765-58-8)、3-(4-氯-2,6-二甲基苯基)-8-甲氧基-1-甲基-2-側氧-1,8-二氮雜螺環[4.5]癸-3-烯-4-基-碳酸乙酯(得自WO 2010/066780 A1,WO 2011151146 A1)(CAS 1229023-00-0)、N-[1-[(6-氯-3-吡啶基)甲基]-2(1H)-亞吡啶基]-2,2,2-三氟-乙醯胺(得自DE 3639877 A1、WO 2012029672 A1)(CAS 1363400-41-2)、[N(E)]-N-[1-[(6-氯-3-吡啶基)甲基]-2(1H)-亞吡啶基]-2,2,2-三氟-乙醯胺(得自WO 2016005276 A1)(CAS 1689566-03-7)、[N(Z)]-N-[1-[(6-氯-3-吡啶基)甲基]-2(1H)-亞吡啶基]-2,2,2-三氟-乙醯胺(CAS 1702305-40-5)、3-內-3-[2-丙氧基-4-(三氟甲基)苯氧基]-9-[[5-(三氟甲基)-2-吡啶基]氧基]-9-氮雜雙環[3.3.1]壬烷(得自WO 2011/105506 A1、WO 2016/133011 A1)(CAS 1332838-17-1)。 Additional active ingredients, such as Afidopyropen, Afoxolaner, Azadirachtin, Benclothiaz, Benzoximate, Bifenazate ( (Bifenazate), Bromolanilide, Bromopropylate, Chinomethionat, Chloroprallethrin, Cryolite, Cyclopramid Cyclaniliprole, Cycloxaprid, Cyhalodiamide, Dicloromezotiaz, Dicofol, E-Methofluthrin, E-Methoxylate Permethrin monomer, Flometoquin, Fluazaindolizine, Fluensulfone, Flufenerim, Flufenoxystrobin, Flufiprole, Fluhexafon , Fluopyram, Fluralaner, Fluxametamide, Fufenozide, Guadipyr, Heptafluthrin, Imidaclothiz ), Iprodione, Kappa-Bifenthrin, K-Stevia (Kappa-Tefluthrin), Lotilaner, Meperfluthrin, Paichongding, Pyridalyl, Pyrifluquinazon, Pyriminostrobin, Spirobudiclofen, Tetrafluoro Tetramethylfluthrin, Tetraniliprole, Tetrachlorantraniliprole, Tigolaner, Tioxazafen, Thiofluoximate, Triflumezopyrim, and Methyliodide; additionally based on Bacillus robustus Preparation (I-1582, BioNeem, Votivo), and the following compounds: 1- {2-fluoro-4-methyl-5-[(2,2,2-trifluoroethyl) sulfinamidino] phenyl } -3- (trifluoromethyl) -1H-1,2,4-triazol-5-amine (available from WO2006 / 043635) (CAS 885026-50-6), {1 '-[(2E)- 3- (4-chlorophenyl) prop-2-en-1-yl] -5-fluorospiro [indole-3,4'-piperidine] -1 (2H) -yl} (2-chloropyridine- 4-yl) methanone (available from WO2003 / 106457) (CAS 637360-23-7), 2-chloro- N- [2- {1-[(2E) -3- (4-chlorophenyl) propane- 2-en-1-yl] piperidin-4-yl} -4- (trifluoromethyl) phenyl] isonicotinamine (available from WO2006 / 003494) (CAS 872999-66-1), 3- (4-chloro-2,6-dimethylphenyl) -4-hydroxy-8-methoxy-1,8-di Spiro [4.5] dec-3-en-2-one (available from WO 2010052161) (CAS 1225292-17-0), 3- (4-chloro-2,6-dimethylphenyl) -8-methoxy 2-Phenyloxy-1,8-diazospiro [4.5] dec-3-en-4-ylethyl carbonate (available from EP 2647626) (CAS-1440516-42-6), 4- (butane 2-alkyn-1-yloxy) -6- (3,5-dimethylpiperidin-1-yl) -5-fluoropyrimidine (available from WO2004 / 099160) (CAS 792914-58-0), PF1364 (available from JP2010 / 018586) (CAS 1204776-60-2), N-[(2E) -1-[(6-chloropyridin-3-yl) methyl] pyridine-2 (1H) -subunit] -2,2,2-trifluoroacetamidamine (available from WO2012 / 029672) (CAS 1363400-41-2), (3 E ) -3- [1-[(6-chloro-3-pyridyl) methyl Phenyl] -2-pyridinyl] -1,1,1-trifluoro-propan-2-one (available from WO2013 / 144213) (CAS 1461743-15-6), N- [3- (benzylamine (Methylamino) -4-chlorophenyl] -1-methyl-3- (pentafluoroethyl) -4- (trifluoromethyl) -1 H -pyrazole-5-carboxamide (available from WO2010 / 051926) (CAS 1226889-14-0), 5-bromo-4-chloro- N- [4-chloro-2-methyl-6- (methylaminomethylmethyl) phenyl] -2- (3 -Chloro-2-pyridyl) pyrazole-3-carboxamide (available from CN103232431) (CAS 1449220-44-3), 4- [5- (3,5-dichlorophenyl) -4,5- Dihydro-5- (trifluoromethyl) -3-iso
Figure TW201945344A_D0142
Oxazolyl] -2-methyl-N- (cis-1-oxo-3-thienyl) benzamide, 4- [5- (3,5-dichlorophenyl) -4,5-di Hydrogen-5- (trifluoromethyl) -3-iso
Figure TW201945344A_D0143
Oxazolyl] -2-methyl-N- (trans-1-oxo-3-thienyl) benzidine and 4-[(5S) -5- (3,5-dichlorophenyl) -4 , 5-dihydro-5- (trifluoromethyl) -3-iso
Figure TW201945344A_D0144
Oxazolyl] -2-methyl-N- (cis-1-oxo-3-thienyl) benzidine (available from WO 2013/050317 A1) (CAS 1332628-83-7), N- [3 -Chloro-1- (3-pyridyl) -1H-pyrazol-4-yl] -N-ethyl-3-[(3,3,3-trifluoropropyl) sulfinamido] propanilamine , (+)- N- [3-chloro-1- (3-pyridyl) -1H-pyrazol-4-yl] -N-ethyl-3-[(3,3,3-trifluoropropyl ) Sulfenyl] propanamide and (-)- N- [3-chloro-1- (3-pyridyl) -1H-pyrazol-4-yl] -N-ethyl-3-[(3 , 3,3-trifluoropropyl) sulfenamidinyl] propanamide (available from WO 2013/162715 A2, WO 2013/162716 A2, US 2014/0213448 A1) (CAS 1477923-37-7), 5- [[(2E) -3-chloro-2-propen-1-yl] amino] -1- [2,6-dichloro-4- (trifluoromethyl) phenyl] -4-[(trifluoro (Methyl) sulfenamidinyl] -1H-pyrazole-3-carbonitrile (available from CN 101337937 A) (CAS 1105672-77-2), 3-bromo-N- [4-chloro-2-methyl- 6-[(methylamino) thiomethyl] phenyl] -1- (3-chloro-2-pyridyl) -1H-pyrazole-5-carboxamide, (Liudaibenjiaxuanan, available from CN 103109816 A ) (CAS 1232543-85-9); N- [4-chloro-2-[[(1,1-dimethylethyl) amino] carbonyl] -6-methylphenyl] -1- (3 -Chloro-2-pyridyl) -3- (fluoromethoxy) -1 H -pyrazole-5-carboxamide (available from WO 2012/034403 A1) (CAS 12682 77-22-0), N- [2- (5-Amino-1,3,4-thiadiazol-2-yl) -4-chloro-6-methylphenyl] -3-bromo-1 -(3-chloro-2-pyridyl) -1 H -pyrazole-5-carboxamide (available from WO 2011/085575 A1) (CAS 1233882-22-8), 4- [3- [2,6 -Dichloro-4-[(3,3-dichloro-2-propen-1-yl) oxy] phenoxy] propoxy] -2-methoxy-6- (trifluoromethyl) pyrimidine (Available from CN 101337940 A) (CAS 1108184-52-6); (2E)-and 2 (Z) -2- [2- (4-cyanophenyl) -1- [3- (trifluoromethyl ) phenyl] ethyl] - N - [4- (difluoromethoxy) phenyl] carbazate Amides (available from CN 101715774 A) (CAS 1232543-85-9) ; 3- (2, 2-dichlorovinyl) -2,2-dimethyl-4- (1H-benzimidazol-2-yl) phenylcyclopropanecarboxylate (available from CN 103524422 A) (CAS 1542271-46-4 ); (4aS) -7-chloro-2,5-dihydro-2-[[((methoxycarbonyl) [4-[(trifluoromethyl) thio] phenyl] amino] carbonyl] indeno [1,2-e] [1,3,4]
Figure TW201945344A_D0145
two
Figure TW201945344A_D0146
-4a (3H) -carboxylic acid methyl ester (available from CN 102391261 A) (CAS 1370358-69-2); 6-deoxy-3- O -ethyl-2,4-di- O -methyl-1 -[ N- [4- [1- [4- (1,1,2,2,2-pentafluoroethoxy) phenyl] -1 H -1,2,4-triazol-3-yl] Phenyl] carbamic acid] -α-L-pyranomannose (available from US 2014/0275503 A1) (CAS 1181213-14-8); 8- (2-cyclopropylmethoxy-4-trifluoromethyl) -Phenoxy) -3- (6-trifluoromethyl
Figure TW201945344A_D0147
-3-yl) -3-azabicyclo [3.2.1] octane (CAS 1253850-56-4), (8-reverse) -8- (2-cyclopropylmethoxy-4-trifluoromethyl) Phenylphenoxy) -3- (6-trifluoromethyl
Figure TW201945344A_D0148
-3-yl) -3-azabicyclo [3.2.1] octane (CAS 933798-27-7), (8-same) -8- (2-cyclopropylmethoxy-4-trifluoromethyl) Phenylphenoxy) -3- (6-trifluoromethyl
Figure TW201945344A_D0149
-3-yl) -3-azabicyclo [3.2.1] octane (available from WO 2007040280 A1, WO 2007040282 A1) (CAS 934001-66-8), N- [3-chloro-1- (3- Pyridyl) -1H-pyrazol-4-yl] -N-ethyl-3-[(3,3,3-trifluoropropyl) thio] -propanilamine (available from WO 2015/058021 A1, WO 2015/058028 A1) (CAS 1477919-27-9) and N- [4- (Aminothiomethyl) -2-methyl-6-[(methylamino) carbonyl] phenyl] -3 -Bromo-1- (3-chloro-2-pyridyl) -1 H -pyrazole-5-carboxamide (available from CN 103265527 A) (CAS 1452877-50-7), 5- (1,3- Dioxalyl-2-yl) -4-[[4- (trifluoromethyl) phenyl] methoxy] -pyrimidine (available from WO 2013/115391 A1) (CAS 1449021-97-9), 3- (4-chloro-2,6-dimethylphenyl) -4-hydroxy-8-methoxy-1-methyl-1,8-diazaspiro [4.5] dec-3-ene 2-one (available from WO 2010/066780 A1, WO 2011/151146 A1) (CAS 1229023-34-0), 3- (4-chloro-2,6-dimethylphenyl) -8-methoxy Methyl-1-methyl-1,8-diazaspiro [4.5] dec-2,4-dione (available from WO 2014/187846 A1) (CAS 1638765-58-8), 3- (4- (Chloro-2,6-dimethylphenyl) -8-methoxy-1-methyl-2- pendant oxygen-1,8-diazaspiro [4.5] dec-3-en-4-yl -Ethyl carbonate (available from WO 2010/066780 A1, WO 2011151146 A1) (CAS 1229023- 00-0), N- [1-[(6-chloro-3-pyridyl) methyl] -2 (1 H ) -pyridinyl] -2,2,2-trifluoro-acetamidine (to From DE 3639877 A1, WO 2012029672 A1) (CAS 1363400-41-2), [N ( E )]-N- [1-[(6-chloro-3-pyridyl) methyl] -2 (1H)- Pyridylene] -2,2,2-trifluoro-acetamidine (available from WO 2016005276 A1) (CAS 1689566-03-7), [N ( Z )]-N- [1-[(6-chloro -3-pyridyl) methyl] -2 (1H) -pyridinyl] -2,2,2-trifluoro-acetamidamine (CAS 1702305-40-5), 3-end-3- [2- Propoxy-4- (trifluoromethyl) phenoxy] -9-[[5- (trifluoromethyl) -2-pyridyl] oxy] -9-azabicyclo [3.3.1] non Alkanes (available from WO 2011/105506 A1, WO 2016/133011 A1) (CAS 1332838-17-1).

可與本發明化合物和組成物混合的安全劑之實例有，例如解草酮(benoxacor)、解毒喹(cloquintocet(-mexyl))、解草胺腈(cyometrinil)、cyprosulfamide、二氯丙烯胺(dichlormid)、解草唑(-乙基)(fenchlorazole-ethyl)、解草啶(fenclorim)、解草胺(flurazole)、氟草肟(fluxofenim)、解草

Figure TW201945344A_D0150
唑(furilazole)、雙苯
Figure TW201945344A_D0151
唑酸(-乙酯)(isoxadifen-ethyl)、吡咯二酸(-二乙酯)(mefenpyr-diethyl)、萘二甲酸酐(naphthalic anhydride)、解草腈(oxabetrinil)、2-甲氧基-N-({4-[(甲基胺甲醯基)胺基]苯基}磺醯基)苯甲醯胺(CAS 129531-12-0)、4-(二氯乙醯基)-1-氧雜-4-氮螺環[4.5]癸烷(CAS 71526-07-3)、2,2,5-三甲基-3-(二氯乙醯基)-1,3-
Figure TW201945344A_D0152
唑啶(CAS 52836-31-4)。 Examples of safeners that can be mixed with the compounds and compositions of the present invention include, for example, benoxacor, cloquintocet (-mexyl), cyometrinil, cyprosulfamide, dichlormid ), Fenchlorazole-ethyl, fenclazole, fenclorim, flurazole, fluofenim, dicamba
Figure TW201945344A_D0150
Furilazole, bisbenzene
Figure TW201945344A_D0151
Isoxadifen-ethyl, isoxadifen-ethyl, mefenpyr-diethyl, naphthalic anhydride, oxabetrinil, 2-methoxy- N-({4-[(methylaminomethylamido) amino] phenyl} sulfoamido) benzamide (CAS 129531-12-0), 4- (dichloroethenyl) -1- Oxa-4-azaspiro [4.5] decane (CAS 71526-07-3), 2,2,5-trimethyl-3- (dichloroethenyl) -1,3-
Figure TW201945344A_D0152
Azodin (CAS 52836-31-4).

可與本發明化合物和組成物混合的除草劑之實例有：乙草胺(acetochlor)、亞喜芬(acifluorfen)、亞喜芬-鈉(acifluorfen-sodium)、苯草醚(aclonifen)、甲草胺(alachlor)、二丙稀草胺(allidochlor)、亞汰草(alloxydim、alloxydim-sodium)、莠滅淨(ametryn)、胺唑草酮(amicarbazone)、先甲草胺(amidochlor)、醯喃橫隆(amidosulfuron)、4-胺基-3-氯-6-(4-氯-2-氟-3-甲基苯 基)-5-氟吡啶-2-羧酸、胺基環丙氯(aminocyclopyrachlor)、胺基環丙氯-鉀、胺基環丙氯-甲基、氯胺吡啶酸(aminopyralid)、殺草強(amitrole)、胺基磺酸銨(ammonium sulfamate)、莎稗磷(anilofos)、橫草靈(asulam)、草脫淨(atrazine)、唑啶草酮(azafenidin)、四唑嘧磺隆(azimsulfuron)、氟丁醯草胺(beflubutamid)、草除靈(benazolin)、乙基草除靈(benazolin-ethyl)、氟草胺(benfluralin)、呋草黃(benfuresate)、苄嘧磺隆(bensulfuron)、免速隆(bensulfuron-methyl)、地散磷(bensulide)、滅草松(bentazone)、雙苯嘧草酮(benzfendizone)、雙環磺草酮(benzobicyclon)、批草酮(benzofenap)、雙環吡喃酮(bicyclopyron)、甲羧除草醚(bifenox)、雙丙胺膦(bilanafos)、雙丙胺膦-鈉(bilanafos-sodium)、雙草醚(bispyribac、bispyribac-sodium)、除草定(bromacil)、溴丁醯草胺(bromobutide)、溴酚肟(bromofenoxim)、溴苯腈(bromoxynil)、溴苯腈-丁酸鹽、-鉀、-庚酸鹽和-辛酸鹽、羥草酮(busoxinone)、丁草胺(butachlor)、氟丙嘧草酯(butafenacil)、抑草磷(butamifos)、丁烯草胺(butenachlor)、比達寧(butralin)、丁苯草酮(butroxydim)、丁草敵(butylate)、唑草胺(cafenstrole)、雙醯草胺(carbetamide)、氟唑草酮(carfentrazone)、乙基克繁草(carfentrazone-ethyl)、草滅平(chloramben)、氯溴隆(chlorbromuron)、伐草克(chlorfenac)、伐草克鈉(chlorfenac-sodium)、燕麥酯(chlorfenprop)、氯甲丹(chlorflurenol)、甲基氯甲丹(chlorflurenol-methyl)、殺草敏(chloridazon)、氯嘧磺隆(chlorimuron)、乙基氯嘧磺隆、氯酞醯亞胺(chlorophthalim)、氯麥隆(chlorotoluron)、氯酞酸二甲酯(chlorthal-dimethyl)、氯磺隆(chlorsulfuron)、吲哚酮(cinidon)、吲哚酮草酯(cinidon-ethyl)、環庚草醚(cinmethylin)、醚磺隆(cinosulfuron)、氯醯草膦(clacyfos)、烯草酮(clethodim)、炔草酸(clodinafop)、炔草酯(clodinafop-propargyl)、異

Figure TW201945344A_D0153
草松(clomazone)、氯甲醯草胺(clomeprop)、二氯吡啶酸(clopyralid)、氯酯磺草酸(cloransulam)、氯酯磺草酸-甲酯(cloransulam-methyl)、節草隆(cumyluron)、胺基氰(cyanamide)、氰草津(cyanazine)、環草敵(cycloate)、cyclopyrimorate、環丙嘧磺隆(cyclosulfamuron)、噻草酮(cycloxydim)、、氰氟草酯(cyhalofop)、氰氟草酯-丁基(cyhalofop-butyl)、環草津(cyprazine)、二、四-地(2,4-D)、二、四-地-丁氧基乙酯(2,4-D-butotyl)、 二、四-地-丁基、二、四-地-二甲基銨、二、四-地-二醇胺、二、四-地-乙基、二、四-地-2-乙基己基、二、四-地-異丁基、二、四-地-異辛基、二、四-地-異丙基銨、二、四-地-鉀、二、四-地-三異丙醇銨及二、四-地-三乙醇胺、2,4-DB、2,4-DB-丁基、2,4-DB-二甲基銨、2,4-DB-異辛基、2,4-DB-鉀和2,4-DB-鈉、殺草隆(daimuron/dymron)、茅草枯(dalapon)、棉隆(dazomet)、正癸醇、甜菜安(desmedipham)、detosyl-pyrazolate(DTP)、麥草畏(dicamba)、敵草腈(dichlobenil)、2-(2,4-二氯苯甲基)-4,4-二甲基-1,2-
Figure TW201945344A_D0154
唑啶-3-酮、2-(2,5-二氯苯甲基)-4,4-二甲基-1,2-
Figure TW201945344A_D0155
唑啶-3-酮、dichlorprop、dichlorprop-P、禾草靈(diclofop)、禾草靈-甲基、禾草靈-P-甲基、雙氯磺草胺(diclosulam)、野燕枯(difenzoquat)、吡氟醯草胺(diflufenican)、氟吡草腙(diflufenzopyr)、氟吡草腙-鈉、
Figure TW201945344A_D0156
唑隆(dimefuron)、呱草丹(dimepiperate)、克草胺(dimethachlor)、戊草津(dimethametryn)、二甲吩草胺(dimethenamid)、精二甲吩草胺(dimethenamid-P)、醚橫隆(dimetrasulfuron)、敵樂胺(dinitramine)；地樂消酚(dinoterb)；草乃敵(diphenamid)；敵草快(diquat)、二溴敵草快(diquat-dibromid)、汰硫草(dithiopyr)；敵草隆(diuron)、DNOC、草藻滅(endothal)、EPTC、伊波卡(eaprocarb)、丁氟消草(ethalfluralin)、胺苯磺隆(ethametsulfuron)、胺苯磺隆(ethametsulfuron-methyl)、乙
Figure TW201945344A_D0157
草酮(ethiozin)、乙呋草黃(ethofumesate)、氯氟草醚乙酯(ethoxyfen)、氯氟醚草乙酯(ethoxyfen-ethyl)、亞速隆(ethoxysulfuron)、乙氧苯草胺(etobenzanid)、F-9600、F-5231，亦即N-{2-氯-4-氟-5-[4-(3-氟丙基)-5-側氧-4,5-二氫-1H-四唑-1-基]苯基}乙磺醯胺、F-7967，亦即3-[7-氯-5-氟-2-(三氟-甲基)-1H-苯并咪唑-4-基]-1-甲基-6-(三氟甲基)嘧啶-2,4(1H,3H)-二酮、芬殺草(fenoxaprop)、芬殺草(fenoxaprop-P)、芬殺草(fenoxaprop-ethyl)、芬殺草(fenoxaprop-P-ethyl)、fenoxasulfone、fenquinotrione、四唑草胺(fentrazamide)、麥草伏(flamprop)、麥草伏異丙酯(flamprop-M-isopropyl)、麥草伏甲酯(flamprop-M-methyl)、啶嘧黃隆(flazasulfuron)、雙氟磺草胺(florasulam)、伏寄普(fluazifop)、伏寄普(fluazifop-P)、伏寄普丁酯(fluazifop-butyl)、伏寄普丁酯(fluazifop-P-butyl)、氟唑磺隆(flucarbazone)、氟唑磺隆-鈉(flucarbazone-sodium),、氟吡磺隆 (flucetosulfuron)、氯乙氟靈(fluchloralin)、氟噻草胺(flufenacet)、氟嗒
Figure TW201945344A_D0158
草酯(flufenpyr)、氟嗒
Figure TW201945344A_D0159
草酯(flufenpyr-ethyl)、唑嘧磺草胺(flumetsulam)、氟烯草酸(flumiclorac)、氟烯草酸戊酯(flumiclorac-pentyl)、丙炔氟草胺(flumioxazin)、氟草隆(fluometuron)、抑草丁、抑草丁-丁酯、抑草丁-甲基銨和抑草丁-甲酯、乙羧氟草醚(fluoroglycofen)、乙羧氟草醚-乙酯、氟丙酸(flupropanate)、氟啶嘧磺隆(flupyrsulfuron)、氟啶嘧磺隆-甲基-鈉、氟啶草酮(fluridone)、氟咯草酮(flurochloridone)、氟氯比(fluroxypyr)、氟氯比(fluroxypyr-meptyl)、呋草酮(flurtamone)、
Figure TW201945344A_D0160
草酸(fluthiacet)、
Figure TW201945344A_D0161
草酸甲酯(fluthiacet-methyl)、氟磺胺草醚(fomesafen)、氟磺胺草醚-鈉、甲醯胺磺隆(foramsulfuron)、殺木膦(fosamine)、固殺草(glufosinate)、固殺草-銨、固殺草-P-鈉、固殺草-P-銨、固殺草-P-鈉、嘉磷塞(glyphosate)、嘉磷塞-銨、嘉磷塞-異丙基銨、嘉磷塞-二銨、嘉磷塞-二甲基銨、嘉磷塞-鉀、嘉磷塞-鈉、和嘉磷塞-三甲基硫鹽、H-9201，亦即O-(2,4-二甲基-6-硝基苯基)O-乙基異丙基胺基硫代磷酸鹽、氟氯吡啶酯(halauxifen)、氟氯吡啶酯-甲酯、氟硝磺醯胺(halosafen)、氯吡嘧磺隆(halosulfuron)、氯吡嘧磺隆-甲基、氟吡禾靈(haloxyfop)、精氟吡禾靈(haloxyfop-P)、氟吡乙禾靈(haloxyfop-ethoxyethyl)、精氟吡乙禾靈(haloxyfop-P-ethoxyethyl)、氟吡甲禾靈(haloxyfop-methyl)、精氟吡甲禾靈(haloxyfop-P-methyl)、環
Figure TW201945344A_D0162
酮(hexazinone)、HW-02亦即1-(二甲氧基磷醯基)乙基-(2,4-二氯苯氧基)乙酸酯、咪草酸(imazamethabenz)、咪草酸甲酯(imazamethabenz-methyl)、甲氧醚磺隆(imazamox)、甲氧醚磺隆-銨、甲咪唑菸酸(imazapic)、甲咪唑菸酸-銨(imazapic-ammonium)、依滅草(imazapyr)、咪唑煙酸-異丙基銨(imazapyr-isopropylammonium)、咪唑喹啉酸(imazaquin)、咪唑喹啉酸-銨、咪唑乙煙酸(imazethapyr)、咪唑乙煙酸-銨、唑吡嘧磺隆(imazosulfuron)、抗倒胺(inabenfide)、茚草酮(indanofan)、茚
Figure TW201945344A_D0163
氟草胺(indaziflam)、碘甲磺隆(iodosulfuron)、碘甲磺隆-甲基-鈉、碘苯腈(ioxynil)、碘苯腈-辛酸、碘苯腈-鉀和碘苯腈-鈉、三唑醯草胺(ipfencarbazone)、異丙樂靈(isopropalin)、異丙隆(isoproturon)、愛速隆(isouron)、異
Figure TW201945344A_D0164
醯草胺(isoxaben)、異
Figure TW201945344A_D0165
唑草酮(isoxaflutole)、特胺靈(karbutilate)、KUH-043，亦即3-({[5-(二氟 甲基)-1-甲基-3-(三氟甲基)-1H-吡唑-4-基]甲基}磺醯基)-5,5-二甲基-4,5-二氫-1,2-
Figure TW201945344A_D0166
唑、凱拓草胺(ketospiradox)、乳氟禾草靈(lactofen)、環草定(lenacil)、利穀隆(linuron)、MCPA、MCPA-丁醯基、MCPA-二甲基銨、MCPA-2-乙基己基、MCPA-異丙基銨、MCPA-鉀和MCPA-鈉、MCPB、MCPB-甲基、MCPB-乙基和MCPB-鈉、二甲四氯丙酸(mecoprop)、二甲四氯丙酸-鈉和二甲四氯丙酸-丁氧基乙酯、二甲四氯丙酸-P、二甲四氯丙酸-P-丁氧基乙酯、二甲四氯丙酸-P-二甲基銨、二甲四氯丙酸-P-2-乙基己基酯和二甲四氯丙酸-P-鉀、苯噻醯草胺(mefenacet)、氯磺醯草胺(mefluidide)、甲磺胺磺隆(mesosulfuron)、甲基甲磺胺磺隆、甲基磺草酮(mesotrione)、甲基苯噻隆(methabenzthiazuron)、威百畝(metam)、
Figure TW201945344A_D0167
唑醯草胺(metamifop)、苯
Figure TW201945344A_D0168
草酮(metamitron)、吡唑草胺(metazachlor)、
Figure TW201945344A_D0169
吡嘧磺隆(metazosulfuron)、甲基苯噻隆(methabenzthiazuron)、甲硫嘧磺隆(methiopyrsulfuron)、methiozolin、甲基異硫氰酸酯、溴穀隆(metobromuron)、異丙甲草胺(metolachlor)、精異丙甲草胺(S-metolachlor)、磺草唑胺(metosulam)、甲氧隆(metoxuron)、
Figure TW201945344A_D0170
草酮(metribuzin)、甲磺隆(metsulfuron)、甲基甲磺隆、禾草敵(molinate)、氯穀隆(monolinuron)、單嘧磺隆(monosulfuron)、單嘧磺隆-酯(monosulfuron-ester)、MT-5950，亦即N-(3-氯-4-異丙基苯基)-2-甲基戊醯胺、NGGC-011、敵草胺(napropamide)、NC-310，亦即[5-(苯甲氧基)-1-甲基-1H-吡唑-4-基](2,4-二氯-苯基)甲酮草不隆(neburon)、煙嘧磺隆(nicosulfuron)、壬酸(nonanoic acid/pelargonic acid)、達草滅(norflurazon)、油酸(脂肪酸)、坪草丹(orbencarb)、嘧苯胺磺隆(orthosulfamuron)、胺磺樂靈(oryzalin)、丙炔
Figure TW201945344A_D0171
草酮(oxadiargyl)、
Figure TW201945344A_D0172
草酮(oxadiazon)、環氧嘧磺隆(oxasulfuron)、
Figure TW201945344A_D0173
草酮(oxaziclomefon)、乙氧氟草醚(oxyfluorfen)、百草枯(paraquat)、百草枯二氯鹽(paraquat dichloride)、克草猛(pebulate)、施得圃(pendimethalin)、五氟磺草胺(penoxsulam)、五氯酚(pentachlorphenol)、環戊
Figure TW201945344A_D0174
草酮(pentoxazone)、烯草胺(pethoxamid)、石油、苯敵草(phenmedipham)、胺氯吡啶酸(picloram)、氟吡醯草胺(picolinafen)、唑啉草酯(pinoxaden)、呱草磷(piperophos)、丙草胺(pretilachlor)、氟嘧磺隆(primisulfuron)、甲基氟嘧磺隆(primisulfuron-methyl)、胺氟樂靈(prodiamine)、 環苯草酮(profoxydim)、撲滅通(prometon)、撲草淨(prometryn)、毒草安(propachlor)、敵稗(propanil)、普拔草(propaquizafop)、撲滅津(propazine)、苯胺靈(propham)、異丙草胺(propisochlor)、丙苯磺隆(propoxycarbazone)、丙苯磺隆-鈉(propoxycarbazone-sodium)、
Figure TW201945344A_D0175
咪唑嘧磺隆(propyrisulfuron)、塊苯醯草胺(propyzamide)、苄草丹(prosulfocarb)、氟磺隆(prosulfuron)、雙唑草腈(pyraclonil)、吡草醚(pyraflufen)、乙基吡草醚(pyraflufen-ethyl)、pyrasulfotole、芐草唑(pyrazolynate(pyrazolate))、吡嘧磺隆(pyrazosulfuron)、吡嘧磺隆-乙基(pyrazosulfuron-ethyl)、節草唑(pyrazoxyfen)、pyribambenz、異丙酯草醚(pyribambenz-isopropyl)、丙酯草醚(pyribambenz-propyl)、嘧苯草肟(pyribenzoxim)、稗草丹(pyributicarb)、嗒草醇(pyridafol)、草特(pyridate)、環酯草醚(pyriftalid)、嘧草醚(pyriminobac)、嘧草醚-甲基(pyriminobac-methyl)、嘧磺苯胺(pyrimisulfan)、嘧草硫醚(pyrithiobac)、嘧草硫醚-鈉(pyrithiobac-sodium)、碸吡草唑(pyroxasulfone)、甲氧磺草胺(pyroxsulam)、二氯喹啉酸(quinclorac)、喹草酸(quinmerac)、莫克草(quinoclamine)、快伏草(quinofop)、快伏草(quizalofop-ethyl)、快伏草(quizalofop-P)、快伏草(quizalofop-P-ethy)、快伏草(quizalofop-P-tefuryl)、玉嘧磺隆(rimsulfuron)、殺芬草(saflufenacil)、西殺草(sethoxydim)、環草隆(siduron)、草滅淨(simazine)、西草淨(simetryn)、SL-261、磺草酮(sulcotrion)、磺醯唑草酮(sulfentrazone)、嘧磺隆(sulfometuron)、甲嘧磺隆(sulfometuron-methyl)、磺胺磺隆(sulfosulfuron)、SYN-523、SYP-249，亦即1-乙氧基-3-甲基-1-側氧丁-3-醯-2-基5-[2-氯-4-(三氟甲基)苯氧基]-2-硝基苯甲酸酯、SYP-300，亦即1-[7-氟-3-側氧-4-(丙-2-炔-1-基)-3,4-二氫-2H-1,4-苯并
Figure TW201945344A_D0176
-6-基]-3-丙基-2-硫咪唑啶-4,5-二酮、2,3,6-TBA、TCA(三氯乙酸)、TCA-鈉、丁唑隆(tebuthiuron)、呋喃磺草酮(tefuryltrione)、環磺酮(tembotrione)、得殺草(tepraloxydim),、特草定(terbacil)、特草靈(terbucarb)、猛殺草(terbuchlor)、甲氧去草淨(terbumeton)、特丁津(terbuthylazin)、去草淨(terbutryn)、欣克草(thenylchlor)、噻草定(thiazopyr)、噻酮磺隆(thiencarbazone)、噻吩磺隆-甲基、噻吩磺隆(thifensulfuron)、噻吩磺隆-甲基、禾草丹(thiobencarb)、tiafenacil、tolpyralate、 苯吡唑草酮(topramezone)、肟草酮(tralkoxydim)、特糠酯酮(triafamone)、野麥畏(triallate)、醚苯磺隆(triasulfuron)、三
Figure TW201945344A_D0177
氟草胺(triaziflam)、苯磺隆(tribenuron)、苯磺隆(tribenuron-methly)、定草酯(triclopyr)、草達津(trietazine)、三氟啶磺隆(trifloxysulfuron)、三氟啶磺隆-鈉(trifloxysulfuron-sodium)、trifludimoxazin、氟樂靈(trifluralin)、氟胺磺隆(triflusulfuron)、氟胺磺隆-甲基、三甲隆(trimeturon)、硫酸脲、滅草猛(vernolate)、XDE-848、ZJ-0862，亦即3,4-二氯-N-{2-[(4,6-二甲氧基嘧啶-2-基)氧基]苯甲基}苯胺，及下列化合物：
Figure TW201945344A_D0178
 Examples of herbicides that can be mixed with the compounds and compositions of the present invention are: acetochlor, acifluorfen, acifluorfen-sodium, aclofen, acetochlor Alachlor, allidochlor, alloxydim, alloxydim-sodium, ametryn, amidcarbazone, amidochlor, sulfan Amidosulfuron, 4-amino-3-chloro-6- (4-chloro-2-fluoro-3-methylphenyl) -5-fluoropyridine-2-carboxylic acid, aminocyclopropyl chloride ( aminocyclopyrachlor), aminocyclopropyl chloride-potassium, aminocyclopropyl chloride-methyl, aminopyralid, amomile, ammonium sulfamate, anilofos ), Asulam, atrazine, azafenidin, azimsulfuron, beflubutamid, benazolin, ethyl Benazolin-ethyl, Benfluralin, Benfuresate, Bensulfuron, Bensulfuron-methyl, Bensulide, Herbicide Pine (bentazone), double Benzfendizone, benzobicyclon, benzofenap, bicyclopyron, bifenox, bilanafos, bispropylamine-sodium (bilanafos-sodium), bispyribac, bispyribac-sodium, bromacil, bromobutide, bromofenoxim, bromoxynil, bromoxynil- Butyrate, -potassium, -heptanoate and -octanoate, busoxinone, butachlor, butafenacil, butamifos, butachlor (butenachlor), butralin, butroxydim, butylate, cabenstrole, carbetamide, carfentrazone, ethyl Carfentrazone-ethyl, chloramben, chlorbromuron, chlorfenac, chlorfenac-sodium, chlorfenprop, chlormethan (chlorflurenol), chlorflurenol-methyl, chloridazon, chlorimuron, ethylchloropyrim Chloroprene, chlorophthalim, chlorotoluron, chlorothal-dimethyl, chlorsulfuron, cinidon, indoxone ( cinidon-ethyl), cinmethylin, cinosulfuron, cloxyfos, clethodim, clodinafop, clodinafop-propargyl, different
Figure TW201945344A_D0153
Clomazone, clomeprop, clopyralid, cloransulam, cloransulam-methyl, cumyluron , Cyanamide, cyanazine, cycloate, cyclopyrimorate, cyclosulfamuron, cycloxydim, cyhalofop, cyhalofop Cyhalofop-butyl, cyprazine, di-, tetra-di (2,4-D), di-, tetra-di-butoxyethyl (2,4-D-butotyl) , Di, tetra-di-butyl, di, tetra-di-dimethylammonium, di, tetra-di-diol amine, di, tetra-di-ethyl, di, tetra-di-2-ethyl Hexyl, di, tetra-di-isobutyl, di, tetra-di-isooctyl, di, tetra-di-isopropylammonium, di, tetra-di-potassium, di, tetra-di-triisopropyl Ammonium alcohol and di, tetra-di-triethanolamine, 2,4-DB, 2,4-DB-butyl, 2,4-DB-dimethylammonium, 2,4-DB-isooctyl, 2, 4-DB-potassium and 2,4-DB-sodium, daimuron / dymron, dalapon, dazomet, n-decanol, desmedipham, detosyl-pyrazolate (DTP ) Dicamba (dicamba), dichlobenil (dichlobenil), 2- (2,4- dichlorobenzyl) -4,4-dimethyl-1,2
Figure TW201945344A_D0154
Oxazidin-3-one, 2- (2,5-dichlorobenzyl) -4,4-dimethyl-1,2-
Figure TW201945344A_D0155
Pyrimidin-3-one, dichlorprop, dichlorprop-P, diclofop, diclofop, methyl, diclofop, diclosulam, difenzoquat ), Diflufenican, diflufenzopyr, diflufenzopyr, sodium,
Figure TW201945344A_D0156
Dimefuron, dimepiperate, dimethachlor, dimethametryn, dimethenamid, dimethenamid-P, dimethenamid dimetrasulfuron, dinitramine; dinoterb; diphenamid; diquat, diquat-dibromid, dithiopyr Diuron, DNOC, endothal, EPTC, eaprocarb, ethalfluralin, ethametsulfuron, ethametsulfuron-methyl B
Figure TW201945344A_D0157
Ethiozin, ethofumesate, ethoxyfen, ethoxyfen-ethyl, ethoxysulfuron, etobenzanid ), F-9600, F-5231, that is, N- {2-chloro-4-fluoro-5- [4- (3-fluoropropyl) -5-side oxygen-4,5-dihydro-1H- Tetrazol-1-yl] phenyl} ethanesulfonamide, F-7967, which is 3- [7-chloro-5-fluoro-2- (trifluoro-methyl) -1H-benzimidazole-4- Propyl] -1-methyl-6- (trifluoromethyl) pyrimidine-2,4 (1H, 3H) -dione, fenoxaprop, fenoxaprop-P, fenoxadi ( fenoxaprop-ethyl), fenoxaprop-P-ethyl, fenoxasulfone, fenquinotrione, fentrazamide, flamprop, flamprop-M-isopropyl, fabaprop (Flamprop-M-methyl), flazasulfuron, florasulam, fluazifop, fluazifop-P, fluazifop- butyl), fluazifop-P-butyl, flucarbazone, flucarbazone-sodium, flucetosulfuron, clofluflune fluchloralin) Flufluacet, flufenacet
Figure TW201945344A_D0158
Flufenpyr, fluta
Figure TW201945344A_D0159
Flufenpyr-ethyl, flumetsulam, flumiclorac, flumiclorac-pentyl, flumioxazin, fluometuron , Buturidine, buturin-butyl ester, buturin-methylammonium and buturin-methyl ester, etflurane-methyl, fluoroglycofen, etflurane-ethyl, flupropanate ), Flupyrsulfuron, flupyrsulfuron-methyl-sodium, fluridone, flurochloridone, fluroxypyr, fluroxypyr -meptyl), flurtamone,
Figure TW201945344A_D0160
Fluthiacet,
Figure TW201945344A_D0161
Fluthiacet-methyl, fomesafen, fomesulfan-sodium, foramsulfuron, fosamine, glufosinate, glufosinate -Ammonium, carbamazepine-P-sodium, carbamazepine-P-ammonium, carbamazepine-P-sodium, glyphosate, carbamazepine-ammonium, carbamazepine-isopropylammonium, chia Phosphine-diammonium, Carboxamidine-dimethylammonium, Carboxamidine-Potassium, Carboxamidine-Sodium, and Carboxamidine-Trimethylsulfide, H-9201, also known as O- (2,4 -Dimethyl-6-nitrophenyl) O-ethylisopropylaminothiophosphate, halofifen, fluorochloropyridyl ester-methyl, halosafen , Clonosulfuron, halosulfuron-methyl, cloflusulfuron-methyl, haloxyfop, haloxyfop-P, haloxyfop-ethoxyethyl, essence Haloxyfop-P-ethoxyethyl, Haloxyfop-methyl, Haloxyfop-P-methyl, Ring
Figure TW201945344A_D0162
Hexazinone, HW-02, also known as 1- (dimethoxyphosphonium) ethyl- (2,4-dichlorophenoxy) acetate, imazamethabenz, methyl imoxalate ( imazamethabenz-methyl), imazamox, imazamox, amazamo, imazapic, imazapic-ammonium, imazapyr, imidazole Imazapyr-isopropylammonium, imazaquin, imazaquin, imazathapyr, imazethapyr, imazethapyr-ammonium, imazosulfuron ), Inabenfide, indanofan, indene
Figure TW201945344A_D0163
Indaziflam, iodosulfuron, iodosulfuron-methyl-sodium, ioxynil, iodobenzonitrile-octanoic acid, iodobenzonitrile-potassium and iodobenzonitrile-sodium, Ipfencarbazone, isopropalin, isoproturon, isouron, isopro
Figure TW201945344A_D0164
Isoxaben, isooxaben
Figure TW201945344A_D0165
Isoxaflutole, karbutilate, KUH-043, that is, 3-({[5- (difluoromethyl) -1-methyl-3- (trifluoromethyl) -1H- Pyrazol-4-yl] methyl} sulfonyl) -5,5-dimethyl-4,5-dihydro-1,2-
Figure TW201945344A_D0166
Azole, ketospiradox, lactofen, lenacil, linuron, MCPA, MCPA-butylamyl, MCPA-dimethylammonium, MCPA-2- Ethylhexyl, MCPA-isopropylammonium, MCPA-potassium and MCPA-sodium, MCPB, MCPB-methyl, MCPB-ethyl and MCPB-sodium, mecoprop, dimethyltetrachloropropane Acid-sodium and dimethyltetrachloropropionic acid-butoxyethyl, dimethyltetrachloropropionic acid-P, dimethyltetrachloropropionic acid-P-butoxyethyl, dimethyltetrachloropropionic acid-P- Dimethylammonium, dimethyltetrachloropropionic acid-P-2-ethylhexyl ester and dimethyltetrachloropropionic acid-P-potassium, mefenacet, mefluidide, Mesosulfuron, mesosulfuron, mesotrione, methabenzthiazuron, metam,
Figure TW201945344A_D0167
Metamifop, benzene
Figure TW201945344A_D0168
Metamitron, metazachlor,
Figure TW201945344A_D0169
Metazosulfuron, methabenzthiazuron, methiopyrsulfuron, methiozolin, methyl isothiocyanate, metobromuron, metolachlor ), S-metolachlor, metosulam, metoxuron,
Figure TW201945344A_D0170
Metribuzin, metsulfuron, metsulfuron, molinate, monolinuron, monosulfuron, monosulfuron-ester ester), MT-5950, that is, N- (3-chloro-4-isopropylphenyl) -2-methylpentanamide, NGGC-011, napropamide, NC-310, that is, [5- (Benzyloxy) -1-methyl-1H-pyrazol-4-yl] (2,4-dichloro-phenyl) methanone neburon, nicosulfuron ), Nonanoic acid / pelargonic acid, norflurazon, oleic acid (fatty acid), orbencarb, orthosulfamuron, oryzalin, propyne
Figure TW201945344A_D0171
Oxadiargyl,
Figure TW201945344A_D0172
Oxadiazon, oxasulfuron,
Figure TW201945344A_D0173
Oxaziclomefon, oxyfluorfen, paraquat, paraquat dichloride, pebulate, pendimethalin, penoxsulam ), Pentachlorphenol, cyclopentyl
Figure TW201945344A_D0174
Pentoxazone, pethoxamid, petroleum, phenmedipham, picloram, picolinafen, pinoxaden, and phosphamid (piperophos), pretilachlor, primisulfuron, primisulfuron-methyl, prodiamine, profoxydim, chlorphenirone (profoxydim) prometon, prometryn, propachlor, propanil, propaquizafop, propazine, propham, propisochlor, propane Propoxycarbazone, propoxycarbazone-sodium,
Figure TW201945344A_D0175
Imidazosulfuron (propyrisulfuron), propyzamide, prosulfocarb, prosulfuron, pyraclonil, pyraflufen, ethylpyramid Ether (pyraflufen-ethyl), pyrasulfotole, pyrazolynate (pyrazolate), pyrazosulfuron, pyrazosulfuron-ethyl, pyrazoxyfen, pyribambenz, isobaric Pyribambenz-isopropyl, pyribambenz-propyl, pyribenzoxim, pyributicarb, pyridafol, pyridate, cyclic esters Pyriftalid, Pyriminobac, Pyriminobac-methyl, Pyrimisulfan, Pyrithiobac, Pyrithiobac-sodium ), Pyroxasulfone, pyroxsulam, quinclorac, quinmerac, quinoclamine, quinofop, quinofop (quizalofop-ethyl), quizalofop-P, quizalofop-P-ethy, quizalofop -P-tefuryl), rimsulfuron, saflufenacil, sethoxydim, siduron, simazine, simetryn, SL -261, sulcotrion, sulfentrazone, sulfometuron, sulfometuron-methyl, sulfosulfuron, SYN-523, SYP-249 , Which is 1-ethoxy-3-methyl-1-oxobut-3-fluoren-2-yl 5- [2-chloro-4- (trifluoromethyl) phenoxy] -2-nitrate Benzoate, SYP-300, that is, 1- [7-fluoro-3-lanthoxy-4- (prop-2-yn-1-yl) -3,4-dihydro-2H-1,4 -Benzo
Figure TW201945344A_D0176
-6-yl] -3-propyl-2-thioimidazolidine-4,5-dione, 2,3,6-TBA, TCA (trichloroacetic acid), TCA-sodium, tebuthiuron, Tefuryltrione, tembotrione, tepraloxydim, terbacil, terbucarb, terbuchlor, methamphetamine terbumeton), terbuthylazin, terbutryn, thenylchlor, thiazopyr, thiencarbazone, thifensulfuron-methyl, thifensulfuron-methyl thifensulfuron, methylthiosulfuron-methyl, thiobencarb, tiafenacil, tolpyralate, topramezone, tramoxydim, triafamone, triallate ), Triasulfuron, triasulfuron
Figure TW201945344A_D0177
Triaziflam, tribenuron, tribenuron-methly, triclopyr, triazazine, trifloxysulfuron, triflusulfuron Trifloxysulfuron-sodium, trifludimoxazin, trifluralin, triflusulfuron, triflusulfuron-methyl, trimeturon, urea sulfate, vernolate, XDE-848, ZJ-0862, which is 3,4-dichloro-N- {2-[(4,6-dimethoxypyrimidin-2-yl) oxy] benzyl} aniline, and the following compounds :
Figure TW201945344A_D0178

植物生長調節劑之實例有：苯丙噻重氮(Acibenzolar)、苯丙噻重氮-S-甲基、5-胺基酮戊酸(5-aminolevulinic acid)、嘧啶醇(ancymidol)、6-苯甲基胺基嘌呤、油菜素內酯(Brassinolide)、兒茶素(catechine)、克美素(chlormequat chloride)、果美生長素(cloprop)、環丙醯草胺(cyclanilide)、3-(環丙-1-烯基)丙酸、亞拉生長素(daminozide)、邁隆(dazomet)、抑芽醇(n-decanol)、敵草克(dikegulac)、敵草克(dikegulac-sodium)、草多索(endothal)、草多索-二鉀、草多索-二鈉、及草多索-單(N,N-二甲基烷基銨)、乙烯利(ethephon)、氟節胺(flumetralin)、芴丁酸(flurenol)、芴丁酸-丁基、調嘧醇(flurprimidol)、氯苯吡脲(forchlorfenuron)、吉貝素(gibberellic acid)、依納素(inabenfide)、吲哚-3-乙酸(IAA)、4-吲哚-3-基丁酸、亞賜圃(isoprothiolane)、撲殺熱(probenazole)、茉莉酸(jasmonic acid)、順丁烯二醯肼(maleic hydrazide)、縮節胺(mepiquat chloride)、1-甲基環丙烯、 茉莉酸甲酯、2-(1-萘基)乙醯胺、1-萘乙酸、2-萘氧基乙酸、硝基酚鹽-混合物、巴克素(paclobutrazol)、N-(2-苯基乙基)-β-丙胺酸、N-苯基酞醯胺酸、調環酸(prohexadione)、調環酸鈣(prohexadione-calcium)、茉莉酸丙酯(prohydrojasmone)、水楊酸、獨腳金內酯(strigolactone)、四氯硝基苯(tecnazene)、噻苯隆(thidiazuron)、三十醇、抗倒酯(trinexapac)、抗倒酯-乙基、tsitodef、烯效唑(uniconazole)、烯效唑-P。 Examples of plant growth regulators are: Acibenzolar, Sulfo-S-methyl, 5-aminolevulinic acid, ancymidol, 6- Benzylaminopurine, brassinolide, catechine, chlormequat chloride, cloprop, cyclanilide, 3- (cyclic Prop-1-enyl) propanoic acid, daminozide, dazomet, n-decanol, dikegulac, dikegulac-sodium, grass Endothal, gadoso-dipotassium, gadoso-diso, and gadoso-mono (N, N-dimethylalkylammonium), ethephon, flumetralin ), Flurenol, butyric acid-butyl, flurprimidol, forchlorfenuron, gibberellic acid, inabenfide, indole-3 -Acetic acid (IAA), 4-indole-3-ylbutyric acid, isoprothiolane, probenazole, jasmonic acid, maleic hydrazide, shrinkage Amine (mepiquat chloride), 1-methylcyclopropane , Methyl jasmonate, 2- (1-naphthyl) acetamidine, 1-naphthylacetic acid, 2-naphthyloxyacetic acid, nitrophenate-mixture, pacobutrazol, N- (2-phenyl (Ethyl) -β-alanine, N-phenylphthalocyanine, prohexadione, prohexadione-calcium, propyl jasmonate (prohydrojasmone), salicylic acid, monopod gold Lactone (strigolactone), tetrachloronitrobenzene (tecnazene), thidiazuron (tidiazuron), triacontanol, trinexapac (trinexapac), trinexyl-ethyl, tsitodef, uniconazole, uniconazole, Monoconazole-P.

方法及用途Method and use

本發明化合物和組成物具有強力的殺微生物活性及/或植物防禦調節潛力。其可用於防治不欲的微生物，例如不欲的真菌和細菌。其特別可用於如更詳細描述於下文的作物保護(防治造成植物罹病的微生物)或保護物料(例如工業物料、木料、儲物)。更特言之，本發明之化合物和組成物可用於保護種子、發芽中的種子、出苗、植物、植物部位、果實、採收物及/或植物生長的土壤免於不欲的微生物。 The compounds and compositions of the present invention have potent microbicidal activity and / or plant defense regulation potential. It can be used to control unwanted microorganisms, such as unwanted fungi and bacteria. It is particularly useful for crop protection (controlling microorganisms that cause plant disease) or to protect materials (eg industrial materials, wood, storage) as described in more detail below. More specifically, the compounds and compositions of the present invention can be used to protect seeds, germinating seeds, emergence, plants, plant parts, fruits, harvests, and / or plant-growing soil from unwanted microorganisms.

因此，本發明進一步係關於用於防治有害微生物，較佳地植物病原性有害真菌、作物保護及物料保護之方法，其中係將至少一種式(I)化合物或包括此化合物的組成物施用於有害的微生物及/或棲地。 Therefore, the present invention further relates to a method for controlling harmful microorganisms, preferably phytopathogenic harmful fungi, crop protection and material protection, wherein at least one compound of formula (I) or a composition comprising the same is applied to harmful Microbes and / or habitats.

本發明進一步係關於至少一種式(I)化合物物或包括此化合物的組成物用於防治有害微生物，較佳地植物病原性有害真菌、作物保護及物料保護之用途。 The invention further relates to the use of at least one compound of formula (I) or a composition comprising the same for controlling harmful microorganisms, preferably phytopathogenic harmful fungi, crop protection and material protection.

本發明亦係關於至少一種式(I)化合物物或包括此化合物的組成物用於處理基因轉殖植物或用於處理種子，較佳地基因轉殖植物種子之用途。 The invention also relates to the use of at least one compound of formula (I) or a composition comprising the same for treating genetically transgenic plants or for treating seeds, preferably genetically transgenic plant seeds.

防治如文中所用係涵蓋保護、治療和根除處理不欲的微生物。不欲的微生物可為病原性細菌、病原性病毒、病原性卵菌或病原性真菌，更特言之植物病原性細菌、植物病原性病毒、植物病原性卵菌或植物病原性真菌。如下文所詳述的，這些植物病原性微生物為造成廣泛植物疾病之致病原。 Control as used herein encompasses protection, treatment and eradication of unwanted microorganisms. Unwanted microorganisms can be pathogenic bacteria, pathogenic viruses, pathogenic oomycetes, or pathogenic fungi, more specifically phytopathogenic bacteria, phytopathogenic viruses, phytopathogenic oomycetes, or phytopathogenic fungi. As detailed below, these phytopathogenic microorganisms are the pathogens that cause a wide range of plant diseases.

更特言之，本發明之化合物和組成物可用作殺真菌劑。就本說明書之目的，術語「殺真菌劑」係指可用於作物保護供防治不欲真菌的化合物或組成物，例如根腫菌綱(Plasmodiophoromycetes)、壺菌綱(Chytridiomycetes)、接合菌綱(Zygomycetes)、子囊菌綱(Ascomycetes)、擔子菌綱(Basidiomycetes)和半知菌(Deuteromycetes)及/或用於防治卵菌綱(Oomycetes)。 More specifically, the compounds and compositions of the present invention are useful as fungicides. For the purposes of this specification, the term "fungicide" refers to compounds or compositions that can be used in crop protection to control unwanted fungi, such as Plasmodiophoromycetes, Chytridiomycetes, Zygomycetes ), Ascomycetes, Basidiomycetes and Deuteromycetes, and / or for the control of Oomycetes.

本發明之化合物和組成物亦可用作為抗細菌劑。特言之，其可用於作物保護，例如用於防治不欲的細菌，例如假單胞菌科(Pseudomonadaceae)、根瘤菌科(Rhizobiaceae)、黃單胞菌科(Xanthomonadaceae)、腸桿菌科(Enterobacteriaceae)、棒狀桿菌科(Corynebacteriaceae)和鏈黴菌科(Streptomycetaceae)。 The compounds and compositions of the present invention can also be used as antibacterial agents. In particular, it can be used for crop protection, for example for controlling unwanted bacteria, such as Pseudomonadaceae, Rhizobaceae, Xanthomonadaceae, Enterobacteriaceae ), Corynebacteriaceae and Streptomycetaceae.

本發明之化合物和組成物可於作物保護上用作為抗病毒劑。例如本發明之化合物和組成物可用於植物病毒之疾病，例如煙草菸草鑲嵌病毒(TMV)、菸草脆裂病毒、矮化病毒(TStuV)、煙草卷葉病毒(VLCV)、煙草脈葉嵌紋病毒(TVBMV)、菸草凋萎病毒(TNDV)、菸草條斑病毒(TSV)、馬鈴薯X病毒(PVX)、馬鈴薯Y、S、M和A病毒、馬鈴薯黃斑紋病毒(PAMV)、馬鈴薯拖把狀頂部病毒(PMTV)、馬鈴薯捲葉病毒(PLRV)、紫花苜蓿鑲嵌病毒(AMV)、胡瓜嵌紋病毒(CMV)、胡瓜綠斑嵌紋病毒(CGMMV)、胡瓜黃病毒(CuYV)、西瓜嵌紋病毒(WMV)、蕃茄斑萎病毒(TSWV)、番茄輪斑病毒(TomRSV)、甘蔗嵌紋病毒(SCMV)、水稻萎縮病毒、水稻縞葉枯病、水稻黑條矮縮病毒、草莓斑駁病毒(SMoV)、草莓鑲脈病毒(SVBV)、草莓輕型黃邊病毒(SMYEV)、草莓皺縮病毒(SCrV)、蠶豆萎凋病毒(BBWV)和甜瓜壞疽斑點病毒(MNSV)。 The compounds and compositions of the present invention can be used as antiviral agents in crop protection. For example, the compounds and compositions of the present invention can be used in diseases of plant viruses, such as tobacco tobacco mosaic virus (TMV), tobacco frittle virus, stunt virus (TStuV), tobacco leaf curl virus (VLCV), tobacco vein mosaic virus (TVBMV), Tobacco Wilt Virus (TNDV), Tobacco Stripe Virus (TSV), Potato X Virus (PVX), Potato Y, S, M and A Viruses, Potato Yellow Spot Virus (PAMV), Potato Mop-Top Virus (PMTV), potato leaf curl virus (PLRV), alfalfa mosaic virus (AMV), courgette mosaic virus (CMV), courgette green spot mosaic virus (CGMMV), courgery yellow virus (CuYV), watermelon mosaic virus ( (WMV), tomato spotted wilt virus (TSWV), tomato round spot virus (TomRSV), sugarcane mosaic virus (SCMV), rice atrophy virus, rice blight, rice black streaked dwarf virus, strawberry mottle virus (SMoV) , Strawberry vein mosaic virus (SVBV), strawberry light yellow edge virus (SMYEV), strawberry crimp virus (SCrV), broad bean wilt virus (BBWV), and melon gangrene spot virus (MNSV).

本發明亦關於防治不欲的微生物，例如不欲的真菌、卵菌和細菌之方法，其係包括將至少一種本發明化合物或至少一種本發明組成物施用於微生物及/或其棲地(施用於植物、植物部位、種子、果實或植物生長的土壤)。 The invention also relates to a method for controlling unwanted microorganisms, such as unwanted fungi, oomycetes and bacteria, which comprises applying at least one compound of the invention or at least one composition of the invention to the microorganism and / or its habitat (application On plants, plant parts, seeds, fruits or soil where plants grow).

典型地，當本發明之化合物和組成物係用於治療或保護方法中供防治植物病原性真菌及/或植物病原性卵菌時，係將其有效和植物相容量施用於植物、植物部位、果實、種子或植物生長的土壤。可用於培育植物的適合基質包括無機和有機基底的基質，例如礦棉，特別是岩棉、真珠石、沙或礫石；有機物質，例如泥炭、松樹皮或鋸屑；及石油基底物質，例如聚合物發泡物或塑料小珠。有效及植物相容量為足以防治或破壞真菌存在或可能出現在田地且對該作物不會牽涉到任何可察覺的植物毒性癥狀。依照所欲防治的真菌、作物類別、作物生長階段、氣候狀況和所使用的個別化合物或組成物，此量可在廣泛的範圍內變化。此量可在熟習本項技術者的能力內，藉由系統性田野試驗來決定。 Typically, when the compounds and compositions of the present invention are used in a method of treatment or protection for controlling phytopathogenic fungi and / or phytopathogenic oomycetes, they are applied to plants, plant parts, The soil on which fruits, seeds or plants grow. Suitable substrates that can be used to cultivate plants include substrates of inorganic and organic substrates, such as mineral wool, especially rock wool, pearlite, sand, or gravel; organic materials such as peat, pine bark, or sawdust; and petroleum-based materials such as polymers Foam or plastic beads. Effective and phytophagic capacity is sufficient to control or destroy the presence or potential of fungi in the field without involving any perceptible symptoms of phytotoxicity to the crop. This amount can vary within a wide range, depending on the fungus to be controlled, the type of crop, the stage of crop growth, the climatic conditions, and the individual compound or composition used. This amount can be determined by systematic field tests within the capabilities of those skilled in the art.

植物和植物部位Plants and plant parts

本發明之化合物和組成物可施用於任何植物或植物部位。 The compounds and compositions of the invention can be applied to any plant or plant part.

植物係指所有的植物和植物群族，例如所欲的及不欲的野生植物或作物植物(包括天然生成的作物植物)。作物植物可為可藉由習用育種和優化方法或藉由生物技術和基因工程方法或這些方法的組合所獲得之植物，包括基因改造植物(GMO或基因轉殖植物)和包括有或無受植物品種權保護之植物品種。 Plants refer to all plants and plant groups, such as desired and unwanted wild plants or crop plants (including naturally occurring crop plants). Crop plants can be plants that can be obtained by conventional breeding and optimization methods, or by biotechnology and genetic engineering methods or a combination of these methods, including genetically modified plants (GMO or genetically modified plants) and including plants Plant varieties protected by variety rights.

基因改造植物(GMO)Genetically Modified Plant (GMO)

基因改造植物(GMO或基因轉殖植物)為其中異源基因已穩定地整合至基因體中之植物。「異源基因」一詞基本上係指在植物外部所提供或組合之基因及導入胞核、葉綠體或粒線體。此基因藉由表現有利的蛋白或多肽，或藉由下調、靜默其他存在植物中的基因(使用例如反義技術、共同抑制技術、RNA干擾-RNAi-技術或微RNA-miRNA-技術)給予該改造的植物新的或改良的農藝或其他性質。位於基因體中的異源基因亦稱為轉殖基因。由其位於植物基因體之特定位置所定義的一轉殖基因係稱為一轉化或轉殖基因品系。 A genetically modified plant (GMO or transgenic plant) is a plant in which a heterologous gene has been stably integrated into the genome. The term "heterologous gene" basically refers to genes provided or combined outside the plant and introduced into the nucleus, chloroplast, or mitochondria. This gene is given by a protein or polypeptide that performs favorably, or by down-regulating, silencing other genes present in the plant (using, for example, antisense technology, co-suppression technology, RNA interference-RNAi-technology or microRNA-miRNA-technology). Modified plants have new or improved agronomic or other properties. Heterologous genes located in the genome are also called transgenic genes. A transgenic gene line defined by its specific location in a plant genome is called a transformed or transgenic line.

植物品種應了解係指具有以正統的育種、基因突變或重組DNA技術所培育出的新特徵(「特質(traits)」)之植物。其可為栽培品種、亞種、生物型及基因型。 Plant varieties should be understood to mean plants that have new characteristics ("traits") developed through orthodox breeding, genetic mutation or recombinant DNA technology. It can be cultivar, subspecies, biotype, and genotype.

植物部位應了解係指植物之所有的地上和地下的植物部位及器官，例如芽、葉、刺、幹、莖、花、果實體、果實、種子、根、塊莖及地下莖。植物部位亦包括採收的物質及無性和生殖性繁殖物質，例如插枝、塊莖、地下莖、接條和種子。 Plant parts should be understood to mean all above-ground and underground plant parts and organs of the plant, such as buds, leaves, thorns, stems, stems, flowers, fruit bodies, fruits, seeds, roots, tubers and underground stems. Plant parts also include harvested material and asexual and reproductive reproduction materials, such as cuttings, tubers, underground stems, splines and seeds.

可依照本發明方法處理的植物係包括下列植物：棉花、亞麻、葡萄、水果、蔬菜，例如薔薇科(Rosaceae sp.)(例如仁果類，如蘋果和梨，以及核果類如杏桃、櫻桃、杏仁及桃子，和漿果類(例如草莓))，茶藨子亞科(Ribesioidae sp.)、胡桃科(Juglandaceae sp.)、樺木科(Betulaceae sp.)、漆樹科(Anacardiaceae sp.)、殼斗科(Fagaceae sp.)、桑科(Moraceae sp.)、木犀科(Oleaceae sp.)、獼猴桃科(Actinidaceae sp.)、樟科(Lauraceae sp.)、芭蕉科(Musaceae sp.)(例如香蕉樹和香蕉園)、茜草科(Rubiaceae sp.)(例如咖啡)、山茶科(Theaceae sp.)、梧桐科(Sterculiceae sp.)、芸香科(Rutaceae sp.)(例如檸檬、柳橙和葡萄柚)；茄科(Solanaceae sp.)(例如番茄)、百合科(Liliaceae sp.)、菊科(Asteraceae sp.)(例如萵苣)、繖形花科(Umbelliferae sp.)、十字花科(Cruciferae sp.)、藜科(Chenopodiaceae sp.)、葫蘆科(Cucurbitaceae sp.)(例如小黃瓜)、蔥科(Alliaceae sp.)(例如韭蔥、洋蔥)、蝶形花科(Papilionaceae sp.)(例如豌豆)；主要的作物植物，例如禾本科(Gramineae sp.)(例如玉米、草皮，穀類例如小麥、黑麥、稻米、大麥、燕麥、小米和黑小麥)，菊科(Asteraceae sp.)(例如向日葵)，十字花科(Brassicaceae sp.)(例如結球白菜、紅球甘藍、青花椰菜、白花椰菜、孢子甘藍、小白菜、球莖甘藍(kohlrabi)、蘿蔔和油菜、芥末、辣根和水芹)、豆科(Fabacae sp.)(例如菜豆、花生)、蝶形花科(例如大豆)、茄科(例如馬鈴薯)、藜科(例如糖用甜菜、飼料甜菜、瑞士甜菜、甜菜根)；花園和林地的有用植物和觀賞植物；以及這些植物各自的基因改造品類。 Plant lines that can be treated according to the method of the present invention include the following plants: cotton, flax, grapes, fruits, vegetables, such as Rosaceae sp. (E.g., nuts such as apples and pears, and stone fruits such as apricots, cherries , Almonds and peaches, and berries (such as strawberries), Ribesioidae sp. , Juglandaceae sp. , Betulaceae sp. , Anacardiaceae sp. , Shells Fagaceae sp. , Moraceae sp. , Oleaceae sp. , Actinidaceae sp. , Lauraceae sp. , Musaceae sp. (E.g. banana Trees and banana orchards), Rubiaceae sp. (E.g. coffee), Theaceae sp. , Sterculiceae sp. , Rutaceae sp. (E.g. lemon, orange and grapefruit ); Solanaceae s p. (E.g. tomato), Liliaceae sp. , Asteraceae sp. (E.g. lettuce), Umbelliferae sp. , Cruciferae sp.), Chenopodiaceae (Chenopodiaceae sp.), Cucurbitaceae (Cucurbitaceae sp.) ( The cucumber), Alliaceae (Alliaceae sp) (e.g. leek, onion), Fabaceae (Papilionaceae sp) (such as peas);.. Major crop plants, such as grasses (Gramineae sp) (for example maize. Turf, cereals such as wheat, rye, rice, barley, oats, millet, and triticale), Asteraceae sp. (E.g., sunflower), Brassicaceae sp. (E.g., cabbage, red cabbage , Broccoli, white cauliflower, spore cabbage, pakchoi, kohlrabi, radish and rape, mustard, horseradish and cress), Fabacae sp. (E.g. bean, peanut), butterfly family (E.g., soybeans), Solanaceae (e.g., potatoes), Chenopodiaceae (e.g., sugar beets, fodder beets, Swiss beets, beetroots); useful and ornamental plants in gardens and woodlands; and genetically modified species of these plants.

可藉由上文所揭示之方法處理的植物和植物品種包括阻抗一或多種生物逆境之植物和植物品種，亦即該植物顯現較佳的抗動物和微生物害蟲，例如抗線蟲、昆蟲、蟎、植物病原性真菌、細菌、病毒及/或類病毒之防禦力。 Plants and plant species that can be treated by the methods disclosed above include plants and plant species that resist one or more biological stresses, that is, the plant appears to be better resistant to animal and microbial pests, such as nematodes, insects, mites, Defense against phytopathogenic fungi, bacteria, viruses and / or viroids.

可藉由上文所揭示之方法處理的植物和植物品種包括該等阻抗一或多種非生物逆境之植物。非生物逆境條件可包括，例如乾旱、低溫暴露、熱暴露、滲透壓、水災、增加的土壤鹽份、增加的礦物暴露、臭氧暴露、強光暴露、限制供應的氮營養素、限制供應的磷營養素、遮蔭迴避。 Plants and plant varieties that can be treated by the methods disclosed above include such plants that resist one or more abiotic stresses. Abiotic stress conditions may include, for example, drought, low temperature exposure, heat exposure, osmotic pressure, flooding, increased soil salinity, increased mineral exposure, ozone exposure, strong light exposure, restricted nitrogen nutrients supply, restricted phosphorus nutrients Avoid shade.

可藉由上文所揭示之方法處理的植物和植物品種包括該等特徵為產量特性提升之植物。該植物中產量提升可能為提高植物生理、生長和發育之結果，例如水利用效率、水保留效率、提升氮利用、提高碳同化、提高光合作用、增加發芽效率和加速成熟。產率可能進一步受到提升的植物建構之影響(在逆境下和非逆境狀況下)，包括，但不限於提早開花、雜交種子產生之開花控制、幼苗活力、植物大小、節的數目和距離、根生長、種子大小、果實大小、莢大小、莢或穗數目、每莢或穗的種子數目、種子重量、提升種子豐滿、降低種子散落、降低莢裂開和抗倒伏性。進一步的產量性狀包括種子組成，例如碳水化合物含量和組成，例如棉花或澱粉、蛋白質含量、油含量和組成、營養價值、減少抗營養化合物、提高可加工性和較佳的儲存穩定性。 Plants and plant varieties that can be treated by the methods disclosed above include plants characterized by improved yield characteristics. The increase in yield in this plant may be the result of improving plant physiology, growth and development, such as water use efficiency, water retention efficiency, nitrogen utilization, carbon assimilation, photosynthesis, germination efficiency and maturation. Yield may be further affected by increased plant construction (under adversity and non-adversity conditions), including, but not limited to, early flowering, flowering control from hybrid seed production, seedling vigor, plant size, number and distance of nodes, roots Growth, seed size, fruit size, pod size, number of pods or ears, number of seeds per pod or ear, seed weight, increased seed plumpness, reduced seed scattering, reduced pod splitting and lodging resistance. Further yield traits include seed composition, such as carbohydrate content and composition, such as cotton or starch, protein content, oil content and composition, nutritional value, reduced anti-nutritional compounds, improved processability, and better storage stability.

可藉由上文所揭示之方法處理的植物和植物品種包括以表現雜交優勢(heterosis)或雜交活力之特性的雜交植物，其通常造成較高產量、活力、健康和對生物和非生物逆境阻抗力之植物和植物品種。 Plants and plant varieties that can be treated by the methods disclosed above include hybrid plants that exhibit characteristics of heterosis or hybrid vigour, which typically result in higher yield, vigor, health, and resistance to biotic and abiotic stress Power plants and plant varieties.

可藉由上文所揭示之方法處理的植物和植物品種(由植物生物技術方法，例如基因工程所獲得)包括除草劑耐受植物，亦即使其耐受一或多種特定的除草劑之植物和植物品種。此等植物可藉由基因轉化或藉由選擇含有賦予此除草劑耐受性之突變的植物來獲得。 Plants and plant varieties (obtained by plant biotechnology methods such as genetic engineering) that can be treated by the methods disclosed above include herbicide-tolerant plants, even plants and plants that are tolerant to one or more specific herbicides and Plant variety. These plants can be obtained by genetic transformation or by selecting plants containing mutations that confer tolerance to this herbicide.

可藉由上文所揭示之方法處理的植物和植物品種(由植物生物技術方法，例如基因工程所獲得)包括抗昆蟲基因轉殖植物，亦即使植物抵 抗特定目標昆蟲攻擊之植物和植物品種。此等植物可藉由基因轉化或藉由選擇含有賦予此昆蟲抗性之突變的植物來獲得。 Plants and plant varieties (obtained by plant biotechnology methods, such as genetic engineering) that can be treated by the methods disclosed above include insect-resistant genetically transgenic plants, even plants that are resistant to attack by specific target insects. These plants can be obtained by genetic transformation or by selecting plants containing mutations that confer resistance to this insect.

可藉由上文所揭示之方法處理的植物和植物品種(由植物生物技術方法，例如基因工程所獲得)包括抗疾病的基因轉殖植物，亦即使植物抵抗特定目標昆蟲攻擊之植物和植物品種。此等植物可藉由基因轉化或藉由選擇含有賦予此昆蟲抗性之突變的植物來獲得。 Plants and plant varieties (obtained by plant biotechnology methods, such as genetic engineering) that can be treated by the methods disclosed above include disease-resistant genetically modified plants, even plants and plant varieties that are resistant to attack by specific target insects . These plants can be obtained by genetic transformation or by selecting plants containing mutations that confer resistance to this insect.

可藉由上文所揭示之方法處理的植物和植物品種(由植物生物技術方法，例如基因工程所獲得)包括耐受非生物逆境之植物和植物品種。此等植物可藉由基因轉化或藉由選擇含有賦予此抗逆性之突變的植物來獲得。 Plants and plant varieties that can be treated by the methods disclosed above (obtained by plant biotechnology methods, such as genetic engineering) include plants and plant varieties that are resistant to abiotic stress. These plants can be obtained by genetic transformation or by selecting plants containing a mutation that confers this resistance.

可藉由上文所揭示之方法處理的植物和植物品種(由植物生物技術方法，例如基因工程所獲得)包括顯現收穫產物數量、品質及/或儲存安定性改變，及/或收穫產物的特定成份性質改變之植物和植物品種。 Plants and plant varieties (obtained by plant biotechnology methods such as genetic engineering) that can be treated by the methods disclosed above include manifesting changes in the quantity, quality, and / or storage stability of the harvested product, and / or specificity of the harvested product Plants and plant varieties with altered properties.

可藉由上文所揭示之方法處理的植物和植物品種(由植物生物技術方法，例如基因工程所獲得)包括，例如具有纖維特性改變的棉花之植物和植物品種。此等植物可藉由基因轉化或藉由選擇含有賦予此改變纖維特性之突變的植物來獲得。 Plants and plant varieties (obtained by plant biotechnology methods, such as genetic engineering) that can be treated by the methods disclosed above include, for example, plants and plant varieties of cotton with altered fiber characteristics. These plants can be obtained by genetic transformation or by selecting plants containing mutations that confer such altered fiber characteristics.

可藉由上文所揭示之方法處理的植物和植物品種(由植物生物技術方法，例如基因工程所獲得)包括，例如具有油特性改變的油菜(oilseed rape)或相關的甘藍(Brassica)植株之植物和植物品種。此等植物可藉由基因轉化或藉由選擇含有賦予此油特性改變之突變的植物來獲得。 Plants and plant varieties (obtained by plant biotechnology methods, such as genetic engineering) that can be treated by the methods disclosed above include, for example, oilseed rape or related Brassica plants with altered oil properties Plants and plant varieties. These plants can be obtained by genetic transformation or by selecting plants containing mutations that impart changes to the characteristics of this oil.

可藉由上文所揭示之方法處理的植物和植物品種(由植物生物技術方法，例如基因工程所獲得)包括，例如具有種子落粒特性改變的油菜或相關的芥菜植株之植物和植物品種。此等植物可藉由基因轉化或藉由選擇含有賦予此種子落粒特性改變之突變的植物來獲得及包括例如具有延遲或降低種子落粒之油菜植株的植物。 Plants and plant varieties (obtained by plant biotechnology methods, such as genetic engineering) that can be treated by the methods disclosed above include, for example, plants and plant varieties of rapeseed or related mustard plants with altered seed-falling characteristics. Such plants can be obtained by genetic transformation or by selecting plants containing mutations that impart changes to the seed's seed-falling characteristics and include, for example, plants with rape plants that delay or reduce seed-dropping.

可藉由上文所揭示之方法處理的植物和植物品種(由植物生物技術方法，例如基因工程所獲得)包括，例如具有改變的後轉譯蛋白修飾模式之菸草植株的植物和植物品種。 Plants and plant varieties (obtained by plant biotechnology methods, such as genetic engineering) that can be treated by the methods disclosed above include, for example, plants and plant varieties of tobacco plants with altered post-translational protein modification patterns.

病原pathogen

可依照本發明處理之真菌疾病病原的非限定實例包括：由白粉病原所造成的疾病，例如布氏白粉菌屬種(Blumeria species)，例如小麥白粉菌(Blumeria graminis)；叉絲單囊殼菌屬種(Podosphaera species)，例如蘋果白澀病菌(Podosphaera leucotricha)；單囊殼菌屬(Sphaerotheca)，例如瓜類白粉病菌(Sphaerotheca fuliginea)；鉤絲殼菌屬種(Uncinula species)，例如葡萄白粉病菌(Uncinula necator)；由銹病病原所造成的疾病，例如梨銹病菌屬種(Gymnosporangium species)，例如蘋果花腐病菌(Gymnosporangium sabinae)；銹病菌屬種(Hemileia species)，例如咖啡銹病菌(Hemileia vastatrix)；層銹菌屬種(Phakopsora species)，例如豆薯層銹菌(Phakopsora pachyrhizi)或山馬蝗層銹菌(Phakopsora meibomiae)；柄銹菌屬種(Puccinia species)，例如小麥葉銹菌(Puccinia recondite)、桿黑銹菌(Puccinia graminis)或小麥條紋銹病(PPuccinia striiformis)；單孢銹菌屬種(Uromyces species)，例如菜豆銹病菌(Uromyces appendiculatus)；由卵菌群類之病原所造成的疾病，例如白銹菌屬種(Albugo species)，例如十字花科白銹菌(Algubo candida)；例如盤梗黴屬種(Bremia species)，例如萵苣露菌病菌(Bremia lactucae)；斜尖孢子菌屬種(Peronospora species)，例如豌豆露菌病菌(Peronospora pisi)或甘藍露菌病菌(P.brassicae)；疫黴菌屬種(Phytophthora species)，例如番茄晚疫病(Phytophthora infestans)；單軸霜黴菌屬種(Plasmopara species)，例如葡萄霜黴菌(Plasmopara viticola)；假霜黴菌屬種(Pseudoperonospora species)，例如啤酒花霜黴菌(Pseudoperonospora humuli)或黃瓜霜黴菌(Pseudoperonospora cubensis)；腐黴菌屬種(Pythium species)，例如終極腐黴菌(Pythium ultimum)； 由下列所造成的葉斑病和葉枯病，例如鏈格菌屬種(Alternaria species)，例如索藍尼氏鏈格菌(Alternaria solani)；尾孢菌屬種(Cercospora species)，例如甜菜尾孢菌(Cercospora beticola)；枝孢菌屬種(Cladiosporum species)，例如黃瓜黑星病菌(Cladiosporium cucumerinum)；旋孢腔菌屬種(Cochliobolus species)，例如禾旋孢腔菌(Cochliobolus sativus)(分生孢子形式：德氏黴(Drechslera)，同義詞：長蠕孢菌(Helminthosporium))或水稻旋孢腔菌(Cochliobolus miyabeanus)；炭疽菌屬種(Colletotrichum species)，例如菜豆炭疽病菌(Colletotrichum lindemuthanium)；棒狀桿孢菌屬棒狀桿孢菌屬種(Corynespora species)，例如多主棒狀桿孢菌(Corynespora cassiicola)；葉斑菌屬種(Cycloconium species)，例如油橄欖孔雀斑病菌(Cycloconium oleaginum)；間座殼屬種(Diaporthe species)，例如柑橘黑點病菌(Diaporthe citri)；痂囊腔菌屬種(Elsinoe species)，例如柑桔痂囊菌(Elsinoe fawcettii)；盤長孢菌屬種(Gloeosporium species)，例如桃炭疽盤長孢菌(Gloeosporium laeticolor)；小叢殼菌屬種(Glomerella species)，例如圍小叢殼菌(Glomerella cingulata)；球座菌屬種(Guignardia species)，例如葡萄球座菌(Guignardia bidwelli)；小球腔菌屬種(Leptosphaeria species)，例如根朽小球腔菌(Leptosphaeria maculans)、穎枯小球腔菌(Leptosphaeria nodorum)；稻瘟病菌屬種(Magnaporthe species)，例如水稻稻瘟菌(Magnaporthe grisea)；微結節菌屬種(Microdochium species)，例如雪黴葉枯病菌(Microdochium nivale)；球腔菌屬種(Mycosphaerella species)，例如禾生球腔菌(Mycosphaerella graminicola)、落花生球腔菌(Mycosphaerella arachidicola)及斐濟球腔菌(Mycosphaerella fijiensis)；暗球腔菌屬種(Phaeosphaeria species)，例如小麥穎枯病菌(Phaeosphaeria nodorum)；核腔菌屬種(Pyrenophora species)，例如圓核腔菌(Pyrenophora teres)或小麥黃斑葉枯病菌(Pyrenophora tritici repentis)；柱隔孢屬種(Ramularia species)，例如(Ramularia collo-cygni)或白斑柱隔孢(Ramularia areola)；喙孢屬種(Rhynchosporium species)，例如黑麥喙孢(Rhynchosporium secalis)；殼針孢屬種(Septoria species)，例如芹菜小殼針孢(Septoria apii)或番茄殼針孢(Septoria lycopersii)；殼多孢菌屬種 (Stagonospora species)，例如小麥穎枯病菌(Stagonospora nodorum)；核瑚菌屬種(Typhula species)，例如肉孢核瑚菌(Typhula incarnate)；黑星菌屬種(Venturia species)，例如蘋果黑星菌(Venturia inaequalis)；由下列所造成之根和莖疾病，例如伏革菌屬種(Corticium species)，例如禾榖伏格菌(Corticium graminearum)；鐮孢菌屬種(Fusarium species)，例如尖孢鐮刀菌(Fusarium oxysporum)；頂囊殼屬種(Gaeumannomyces species)，例如禾頂囊殼菌(Gaeumannomyces graminis)；根瘤菌屬種(Plasmodiophora species)，例如十字花科根腫菌(Plasmodiophora brassicae)；絲核菌屬種(Rhizoctonia species)，例如立枯絲核菌(Rhizoctonia solani)；掃枝黴屬種(Sarocladium species)例如稻葉鞘腐敗病菌(Sarocladium oryzae)；小菌核屬種(Sclerotium species)，例如稻腐小核菌(Sclerotium oryzae)；眼斑病菌屬種(Tapesia species)，例如針形眼斑病菌(Tapesia acuformis)；根串株黴屬種(Thielaviopsis species)，例如煙草根黑腐病菌(Thielaviopsis basicola)；由下列所造成之穗和花序(包括玉米穗軸)疾病，例如鏈格菌屬種(Alternaria species)，例如鏈格菌屬(Alternaria spp.)；麴菌屬種(Aspergillus species)，例如黃麴菌(Aspergillus flavus)；枝孢菌屬種(Cladosporium species)，例如芽枝枝孢菌(Cladosporium cladosporioides)；麥角菌屬種(Claviceps species)，例如紫麥角菌(Claviceps purpurea)；鐮刀菌屬種(Fusarium species)，例如黃色鐮刀菌(Fusarium culmorum)；赤黴菌屬種(Gibberella species)，例如玉米赤黴(Gibberella zeae)；格氏黴屬種(Monographella species)，例如雪腐格氏黴(Monographella nivalis)；殼多孢菌屬種(Stagonospora species)，例如小麥穎枯病菌(Stagonospora nodorum)；由黑穗病真菌所造成之疾病，例如軸黑粉菌屬種(Sphacelotheca species)，例如高粱絲軸黑粉菌(Sphacelotheca reiliana)；腥黑粉菌屬種(Tilletia species)，例如網腥黑穗病菌(Tilletia caries)或矮腥黑穗病菌(Tilletia.controversa)；條黑粉菌屬種(Urocystis species)，例如隱條黑粉菌(Urocystis occulta)；黑粉菌屬種(Ustilago species)，例如裸黑粉菌(Ustilago nuda)； 由下列所造成之果實腐爛，例如麴菌屬種(Aspergillus species)，例如黃麴菌(Aspergillus flavus)；灰黴屬種(Botrytis species)，例如貴腐菌(Botrytis cinerea)；褐腐病菌屬種(Monilinia species)，例如核果褐腐病菌(Monilinia laxa)；青黴菌屬種(Penicillium species)，例如擴展青黴菌(Penicillium expansum)或紫青黴菌(Penicillium purpurogenum)；根黴屬種(Rhizopus species)，例如匍枝根黴(Rhizopus stolonifer)；核盤菌屬種(Sclerotinia species)，例如(Sclerotinia sclerotiorum)；輪刺孢菌屬種(Verticilium species)，例如黑白輪枝菌(Verticilium alboatrum)；由下列所造成之種子及土媒腐病和枯病，以及幼苗之疾病，例如鏈格菌屬種(Alternaria species)，例如十字花科黑斑病菌(Alternaria brassicicola)；絲囊黴屬種(Aphanomyces species)，例如根腐絲囊黴(Aphanomyces euteiches)；殼二胞菌屬種(Ascochyta species)，例如扁豆二胞菌(Ascochyta lentis)；麴菌屬種(Aspergillus species)，由例如黃麴菌(Aspergillus flavus)；枝孢菌屬種(Cladosporium species)，例如多主枝孢菌(Cladosporium herbarum)；旋孢腔菌屬種(Cochliobolus species)，例如禾旋孢腔菌(Cochliobolus sativus)(分生孢子形式：德氏黴(Drechslera)，雙孔孢菌(Bipolaris)同義詞：長蠕孢菌(Helminthosporium))；炭疽菌屬種(Colletotrichum species)，例如仙人掌炭疽刺盤孢菌(Colletotrichum coccodes)；鐮刀菌屬種(Fusarium species)，例如黃色鐮刀菌(Fusarium culmorum)；赤黴菌屬種(Gibberella species)，例如玉米赤黴(Gibberella zeae)；殼球孢菌屬種(Macrophomina species)，例如菜豆殼球孢菌(Macrophomina phaseolina)；微座孢菌屬種(Microdochium species)，例如雪腐微座孢(Microdochium nivale)；格氏黴屬種(Monographella species)，例如雪腐格氏黴(Monographella nivalis)；青黴菌屬種(Penicillium species)，例如擴展青黴菌(Penicillium expansum)；莖點黴菌屬種(Phoma species)，例如黑脛莖點黴(Phoma lingam)；擬莖點黴屬種(Phomopsis species)，例如大豆擬莖點黴(Phomopsis sojae)；疫黴屬種(Phytophthora species)，例如惡疫黴(Phytophthora cactorum)；核腔菌屬種(Pyrenophora species)，例如大麥核腔菌(Pyrenophora graminea)；梨孢黴菌屬種(Pyricularia species)，例如稻瘟病 菌(Pyricularia oryzae；腐黴菌屬種(Pythium species)，例如終極腐黴(Pythium ultimum)；絲核菌屬種(Rhizoctonia species)，例如立枯絲核菌(Rhizoctonia solani)；根黴菌屬種(Rhizopus species)，例如稻根黴菌(Rhizopus oryzae)；菌核屬種(Sclerotium species)，例如白絹病菌(Sclerotium rolfsii)；殼針孢屬種(Septoria species)，例如穎枯殼針孢(Septoria nodorum)；核瑚菌屬種(Typhula species)，例如肉孢核瑚菌(Typhula incarnata)；輪枝黴屬種(Verticilium species)，例如大麗輪枝菌(Verticillium dahliae)；由下列所造成之癌、癭和簇葉病，例如叢赤殼菌屬種(Nectria species)，例如仁果癌叢赤殼菌(Nectria galligena)；由下列所造成之枯萎病，例如輪枝黴屬種(Verticilium species)，例如長輪枝菌(Verticillium longisporum)；鐮刀菌屬種(Fusarium species)，例如尖孢鐮刀菌(Fusarium oxysporum)；由下列所造成之葉子、花和果實之變形，例如外擔菌屬種(Exobasidium species)，例如壞損外擔菌(Exobasidium vexans)；外囊菌屬種(Taphrina species)，例如畸形外囊菌(Taphrina deformans)；由下列所造成之木本植物之退化性疾病：例如伊斯卡菌屬種(Esca species)，例如厚垣孢普可尼亞菌(Phaemoniella clamydospora)和(Phaeoacremonium aleophilum)及地中海藍孢孔菌(Fomitiporia mediterranea)；靈芝屬種(Ganoderma species)，例如狹長孢靈芝(Ganoderma boninense)；由下列所造成之植物塊莖之疾病，例如絲核菌屬種(Rhizoctonia species)，例如立枯絲核菌(Rhizoctonia solani)；長蠕孢黴屬種(Helminthosporium species)，例如馬鈴薯屑病菌(Helminthosporium solani)；由細菌病原所造成的疾病，例如黃單胞菌屬種(Xanthomonas species)，例如葉枯病菌(Xanthomonas campestris pv.Oryzae)；假單胞菌屬種(Pseudomonas species)，例如丁香假單胞菌黃瓜致病變種(Pseudomonas syringae pv.Lachrymans)；伊文氏桿菌屬種(Erwinia species)，例如梨火疫病菌(Erwinia amylovora)；韌皮桿菌屬種(Liberibacter species)，例如亞洲柑桔黃龍病菌(Liberibacter asiaticus)；木質桿菌屬種(Xyella species)，例如葉緣焦枯菌 (Xylella fastidiosa)；雷爾氏菌屬種(Ralstonia species)，例如青枯病菌(Ralstonia solanacearum)；Dickeya屬種(Dickeya species)，例如立枯絲核病菌(Dickeya solani)；棒桿菌屬種(Clavibacter species)，例如輪腐病菌(Clavibacter michiganensis)；鏈黴菌屬種(Streptomyces species)，例如瘡痂病鏈黴菌(Streptomyces scabies)。 Non-limiting examples of fungal disease pathogens that can be treated in accordance with the present invention include: diseases caused by powdery mildew, such as Blumeria species, such as Blumeria graminis ; Podosphaera species, such as Podosphaera leucotricha ; Sphaerotheca , such as Sphaerotheca fuliginea ; Uncinula species, such as grape powder Uncinula necator ; diseases caused by rust pathogens, such as Gymnosporangium species, such as Gymnosporangium sabinae ; Hemileia species, such as coffee rust emileia vastatrix ); Phakopsora species, such as Phakopsora pachyrhizi or Phakopsora meibomiae ; Puccinia species, such as wheat leaf rust Fungus ( Puccinia recondite) , Puccinia graminis , or wheat stripe rust ( PPuccinia striiformis ) ; Uromyces species, such as Uromyces appendiculatus ; diseases caused by pathogens of the oomycete , such as Albugo species, such as Cruciferous white rust ( Algubo candida ); for example, Bremia species, such as Bremia lactucae ; Peronospora species, such as Peronospora pisi or Brassica rapae P. brassicae ; Phytophthora species, such as Phytophthora infestans ; Plasmopara species, such as Plasmopara viticola ; Phytophthora species (Pseudoperonospora species), e.g. downy mildew of hops (Pseudoperonospora humuli) or cucumber downy mildew (Pseudoperonospora cubensis); species Pythium (Pythium species), for example, Pythium fungi (Pythium ultimum); caused by the following leaf spot and leaf Blight, such as Alternaria species, such as Alternaria solani ; Cercospora species, such as Cercospora beticola ; Cladiosporum species, such as Cladiosporium cucumerinum; Cochliobolus species , For example, Cochliobolus sativus (conidia form: Drechslera , synonym: Helminthosporium ) or Cochliobolus miyabeanus ; anthrax species ( Colletotrichum species), such as Colletotrichum lindemuthanium ; Corynespora species, such as Corynespora cassiicola ; and Leaf spot bacteria ( Cycloconium species), such as Cycloconium oleaginum ; Diaporthe species, such as Diaporthe citri ; Elsinoe species, such as Citrus capsicum Elsinoe fawcettii ; Gloeosporium species, such as Gloeosporium laeticolor ); Glomerella species, such as Glomerella cingulata ; Guignardia species, such as Guignardia bidwelli ; Micrococcus species ( Leptosphaeria species), such as Leptosphaeria maculans , Leptosphaeria nodorum ; Magnaporthe species, such as Magnaporthe grisea ; micronodules Microdochium species, such as Microdochium nivale ; Mycosphaerella species, such as Mycosphaerella graminicola , Mycosphaerella arachidicola , and Fiji ball Mycosphaerella fijiensis ; Phaeosphaeria species, such as Phaeosphaeria nodorum ; Pyrenophora species, such as Pyrenophora teres or wheat macula Leaf blight ( Pyrenophora tritici repentis ); Ramularia species, such as ( Ramularia col lo-cygni ) or Ramularia areola ; Rhynchosporium species, such as Rhynchosporium secalis ; Septoria species, such as Celery Septoria apii ) or Septoria lycopersii ; Stagonospora species, such as Stagonospora nodorum ; Typhula species, such as S. sarcocystis ( Typhula incarnate ); Venturia species, such as Venturia inaequalis ; Root and stem diseases caused by, for example, Corticium species, such as Gramineae Corticium graminearum ; Fusarium species, such as Fusarium oxysporum ; Gaeumannomyces species, such as Gaeumannomyces graminis ; Rhizobium Plasmodiophora species, such as Plasmodiophora brassicae ; Rhizoctonia species, such as Rhizoct onia solani ); Sarocladium species such as Sarocladium oryzae ; Sclerotium species such as Sclerotium oryzae ; Sclerotium oryzae Tapesia species), such as Tapesia acuformis ; Thielaviopsis species, such as tobacco root black rot, Thielaviopsis basicola ; spikes and inflorescences (including corn cobs) caused by ) Diseases, such as Alternaria species, such as Alternaria spp . ; Aspergillus species, such as Aspergillus flavus ; Cladosporium species, such as Cladosporium cladosporioides ; Claviceps species, such as Claviceps purpurea ; Fusarium species, such as Fusarium culmorum ); Gibberella species, such as Gibberella zeae ; Monographella species, such as Grignard snow rot Monographella nivalis ; Stagonospora species, such as Stagonospora nodorum ; diseases caused by smut fungi, such as Sphacelotheca species, such as Article Ustilago species; Ustilago sorghum wire shaft (Sphacelotheca reiliana); Tilletia sp (Tilletia species), bacteria e.g. bunt (Tilletia caries), or dwarf bunt bacteria (Tilletia.controversa) ( Urocystis species), such as Urocystis occulta ; Ustilago species, such as Ustilago nuda ; fruit rot caused by, for example, Puccinia species ( Aspergillus species), such as Aspergillus flavus ; Botrytis species, such as Botrytis cinerea ; Monilinia species, such as stone fruit brown rot fungus ( Monilinia laxa ) ; Penicillium species, such as Penicillium expansum or Penicillium purpurogenum ; Rhizopus spec ies), such as Rhizopus stolonifer ; Sclerotinia species, such as ( Sclerotinia sclerotiorum ); Verticilium species, such as Verticilium alboatrum ; Seed and soil-borne rot and blight caused by the following, and diseases of seedlings, such as Alternaria species, such as Alternaria brassicicola ; Aphanomyces species), such as Aphanomyces euteiches ; Ascochyta species, such as Ascochyta lentis ; Aspergillus species, such as Aspergillus flavus ); Cladosporium species, such as Cladosporium herbarum ; Cochliobolus species, such as Cochliobolus sativus (conidia) form: Drechslera (Drechsl era), two holes cinerea (Bipolaris) synonym: Helminthosporium (Helminthosporium)); Colletotrichum species (Colletotrichum species), The cactus anthrax bacteria Colletotrichum (Colletotrichum coccodes); Fusarium species (Fusarium species), for example, yellow Fusarium (Fusarium culmorum) bacteria; Gibberella species (Gibberella species), e.g. zearalenone (Gibberella zeae); ball shell genus species (Macrophomina species), for example, a ball shell bean cinerea (Macrophomina phaseolina); Alternaria sp micro seat (Microdochium species), for example, snow rot Fusarium micro seat (Microdochium nivale); Grignard Geotrichum species (Monographella species ), Such as Monographella nivalis ; Penicillium species, such as Penicillium expansum ; Phoma species, such as Phoma lingam ); Phomopsis species, such as Phomopsis sojae ; Phytophthora species, such as Phytophthora cactorum ; Pyrenophora species ), such as barley Pyrenophora (Pyrenophora graminea); Pyricularia genus Streptomyces species (Pyricularia species), for example, rice blast fungus (Pyricularia or yzae; species Pythium (Pythium species), for example, Pythium ultimum (Pythium ultimum); Rhizoctonia species (Rhizoctonia species), for example, Rhizoctonia solani (Rhizoctonia solani); Rhizopus species (Rhizopus species), For example, Rhizopus oryzae ; Sclerotium species, such as Sclerotium rolfsii ; Septoria species, such as Septoria nodorum ; Typhula species, such as Typhula incarnata ; Verticilium species, such as Verticillium dahliae ; cancers, slugs, and clusters caused by Leaf disease, such as Nectria species, such as Nectria galligena ; Fusarium wilt caused by, for example, Verticilium species, for example Verticillium longisporum ; Fusarium species, such as Fusarium oxysporum ; deformation of leaves, flowers, and fruits caused by, for example, exophytes Species (Exobasidium species), e.g. bacterial outer supporting corruption (Exobasidium vexans); sp external capsule (Taphrina species), e.g. deformities bladder bacteria (Taphrina deformans); a woody plant of the following caused degenerative diseases: For example, Esca species, such as Phaemoniella clamydospora and Phaeoacremonium aleophilum , and Fomitiporia mediterranea ; Ganoderma species, such as Ganoderma boninense ; diseases of tubers of plants caused by, for example, Rhizoctonia species, such as Rhizoctonia solani ; Helminthosporium species , Such as Helminthosporium solani ; diseases caused by bacterial pathogens, such as Xanthomonas species, such as Xanthomonas campestris pv. Oryzae ; Pseudomonas species), such as Pseudomonas syringae pv . Lachrymans ; Evans Erwinia species, such as Erwinia amylovora ; Liberibacter species, such as Liberibacter asiaticus ; Xyella species, such as leaf bacteria edge scorch (Xylella fastidiosa); Ralstonia sp (Ralstonia species), e.g. bacterial wilt (Ralstonia solanacearum) bacteria; Dickeya species (Dickeya species), e.g. Rhizoctonia germ (Dickeya solani); genus Corynebacterium Clavibacter species, such as Clavibacter michiganensis ; Streptomyces species, such as Streptomyces scabies .

大豆疾病：     Soy disease:    

由下列所造成之葉、莖、莢和種子的真菌疾病：鏈格菌葉斑病(鏈格菌類黑鏈格菌(atrans tenuissima))、炭疽病(赤葉枯刺盤孢菌(Colletotrichum gloeosporoides dematium var.truncatum))、褐斑(大豆褐紋殼針孢(Septoria glycines)、尾孢菌(cercospora)葉斑及枯萎(菊池尾孢(Cercospora kikuchii)、笄黴葉枯病(三孢漏斗笄黴(Choanephora infundibulifera trispora(同義詞))、疏毛核菌黴葉斑(疏毛核菌黴(dactuliophora glycines))、露菌病(大豆露菌病菌(Peronospora manshurica))、德氏黴枯萎病(大豆德氏黴球(Drechslera glycini))、蛙眼葉斑病(大豆尾孢菌(Cercospora sojina))、小光腔菌葉斑(小光腔菌(Leptosphaerulina trifolii))、葉點黴葉班(大豆灰星葉點病菌(Phyllosticta sojaecola))、莢枯病和莖枯病(Phomopsis sojae)、白粉病(擴散叉絲殼菌(Microsphaera diffusa))、棘殼孢葉斑病(大豆棘殼孢(Pyrenochaeta glycines))、菌核地上部分枯萎病(rhizoctonia aerial)、葉枯病(foliage)及立枯病(web blight)(立枯絲核菌(Rhizoctonia solani))、銹病(豆薯層銹菌(Phakopsora pachyrhizi)、山馬蝗層銹菌(Phakopsora meibomiae))、痂病(Sphaceloma glycines)、葡柄黴菌葉枯病(葡柄黴菌(Stemphylium botryosum))、猝死症(鐮刀菌(Fusarium virguliforme))、靶斑病(多主棒孢黴(Corynespora cassiicola))。 Fungal diseases of leaves, stems, pods and seeds caused by: Streptococcus leaf spot ( atrans tenuissima ), anthracnose ( Colletotrichum gloeosporoides dematium var.truncatum )), brown spot ( Septoria glycines ), cercospora leaf spot and wilt ( Cercospora kikuchii ) ( Choanephora infundibulifera trispora (synonym)), Sclerotinia sclerotiorum ( dactuliophora glycines ), dermatophytosis ( Peronospora manshurica ), Dermatophyte blight Drechslera glycini ), frog eye leaf spot ( Cercospora sojina ), leaf spot ( Leptosphaerulina trifolii ), leaf spot mold (soy ash) Phyllosticta sojaecola ), pod blight and stem blight ( Pomopsis sojae ), powdery mildew ( Microsphaera diffusa ), echinoderma leaf spot ( Pyrenochaeta glycines )), Part of the sclerotia on the ground Wilt (rhizoctonia aerial), leaf blight (foliage) and web blight ( Rhizoctonia solani ), rust (Phakopsora pachyrhizi ), mountain horse locust layer rust Phakopsora meibomiae ), Sphaceloma glycines , Stemphylium botryosum ), Sudden Death ( Fusarium virguliforme ), Target spot disease ( Corynespora polycephala ) ( Corynespora cassiicola )).

下列所造成之根和莖基部的真菌疾病：例如黑根腐病(叢赤殼菌(Calonectria crotalariae))、芽腐病(殼球孢菌(Macrophomina phaseolina))、鐮刀菌枯萎病或枯萎、根腐及莢和領腐病(尖孢鐮刀菌(Fusarium oxysporum)、長直喙鐮刀菌(Fusarium orthoceras)、半裸鐮刀菌(Fusarium semitectum)、木賊鐮刀菌(Fusarium equiseti))、蓮孢黴根腐病(鳳眼蓮孢黴(Mycoleptodiscus terrestris))、新赤殼菌(neocosmospora)(Neocosmopspora vasinfecta)、莢和莖 枯萎(莖潰瘍病菌(Diaporthe phaseolorum))、莖潰瘍病(大豆北方莖潰瘍病菌(Diaporthe phaseolorum var.caulivora))、疫黴腐病(大豆疫病菌(Phytophthora megasperma))、褐莖腐病(大豆莖褐腐病菌(Phialophora gregata)、腐黴性腐病(瓜果腐黴(Pythium aphanidermatum)、畸雌腐黴(Pythium irregulare)、德氏腐黴(Pythium debaryanum)、群結腐黴(Pythium myriotylum)、終極腐黴(Pythium ultimum))、絲核菌根腐、莖腐和猝倒病(立枯絲核菌(Rhizoctonia solani))、菌核性莖腐病(菌核病菌(Sclerotinia sclerotiorum))、菌核性白絹病(齊整小菌核菌(Sclerotinia rolfsii))、根串珠黴根腐病(根串珠黴(Thielaviopsis basicola))。 Fungal diseases of the roots and stem bases such as: black root rot ( Calonectria crotalariae ), bud rot ( Macrophomina phaseolina ), Fusarium wilt or wilt, roots Rot and Pods and Collar Rot ( Fusarium oxysporum , Fusarium orthoceras , Fusarium semitectum , Fusarium equiseti ), Pseudomonas root rot ( Mycoleptodiscus terrestris ), neocosmospora ( Neocosmopspora vasinfecta ), pod and stem wilt ( diaporthe phaseolorum ), stem ulcer ( diaporthe phaseolorum var.caulivora )), Phytophthora sojae ( Phytophthora megasperma ), Brown stalk rot ( Phyophophora gregata ), Pythium rot (Pythium aphanidermatum ), Pythium irregulare (Pythium irregulare), delemar Pythium (Pythium debaryanum), Pythium group junction (Pythium myriotylum), Pythium ultimum (Pythium ultimum)), Rhizoctonia rot mycorrhiza, stem And damping off (Rhizoctonia solani (Rhizoctonia solani)), sclerotia of stem rot (Sclerotinia sclerotiorum (Sclerotinia sclerotiorum)), sclerotia of southern blight (Sclerotinia small neat (Sclerotinia rolfsii)), Rhizopus rhizogenes ( Thelaviopsis basicola ).

黴菌毒素Mycotoxins

此外，本發明之化合物和組成物可降低收穫物和食品及從其所製備的飼料中之黴菌毒素含量。黴菌毒素包括，特別是，但不僅限於下列：去氧雪腐鐮刀菌烯醇(deoxynivalenol)(DON)、雪腐鐮刀菌烯醇(nivalenol)、15-Ac-DON、3-Ac-DON、T2-和HT2-毒素、伏馬菌素(fumonisins)、玉米赤黴烯酮(zearalenon)、串珠鐮刀菌素(moniliformin)、鏈菌素(fusarin)、雙乙酸基草鐮刀菌醇(diaceotoxyscirpenol)(DAS)、白僵菌素(beauvericin)、恩廉孢菌素(enniatin)、層出鐮孢菌素(fusaroproliferin)、鐮刀菌醇(fusarenol)、赭曲毒素(ochratoxins)、展青黴素(patulin)、麥角類生物鹼(ergot alkaloids)和黃麴毒素(aflatoxins)，其可由例如下列真菌所產生：鐮刀菌屬種(Fusarium spec.)，例如銳頂鐮刀菌(F.acuminatum)、禾穀鐮刀菌(F.asiaticum)、燕麥鐮刀菌(F.avenaceum)、庫威鐮刀菌(F.crookwellense)、黃色鐮刀菌(F.culmorum)、禾穀鐮刀菌(F.graminearum)(玉米赤黴)、術賊鐮刀菌(F.equiseti)、藤倉鐮刀菌(F.fujikoroi)、香蕉鐮刀菌(F.musarum)、尖孢鐮刀菌(F.oxysporum)、再育鐮刀菌(F.proliferatum)、梨孢鐮刀菌(F.poae)、(F.pseudograminearum)、接骨木鐮刀菌(F.sambucinum)、藤草鐮刀菌(F.scirpi)、半裸鐮刀菌(F.semitectum)、茄病鐮刀菌(F.solani)、擬枝孢鐮刀菌(F.sporotrichoides)、F.langsethiae、膠孢鐮刀菌(F.subglutinans)、三線鐮刀菌(F.tricinctum)、串珠鐮刀菌(F.verticillioides)，以及由麯菌屬種(Aspergillus spec.)所產生，例如黃 麴菌(A.flavus)、寄生麯菌(A.parasiticus)、紅綬麯菌(A.nomius)、赭麯菌(A.ochraceus)、棒麯菌(A.clavatus)、土麯菌(A.terreus)、雜色麯菌(A.versicolor)，青黴菌屬種(Penicillium spec.)，例如純綠青黴(P.verrucosum)、鮮綠青黴(P.viridicatum)、橘青黴(P.citrinum)、擴展青黴(P.expansum)、棒形青黴(P.claviforme)、婁地青黴(P.roqueforti)，麥角菌屬種(Claviceps spec.)，例如紫麥角菌(C.purpurea)、梭狀麥角菌(C.fusiformis)、雀稗麥角菌(C.paspali)、非洲麥角菌(C.africana)，葡萄穗黴屬種(Stachybotrys spec.)及其他。 In addition, the compounds and compositions of the present invention can reduce mycotoxins in harvests and foods and feeds prepared from them. Mycotoxins include, in particular, but are not limited to, the following: deoxynivalenol (DON), nivalenol, 15-Ac-DON, 3-Ac-DON, T2 -And HT2-toxin, fumonisins, zearalenon, moniliformin, fusarin, diceotoxyscirpenol (DAS) ), Beauvericin, enniatin, fusaroproliferin, fusarenol, ochratoxins, patulin, wheat Ergot alkaloids and aflatoxins can be produced by, for example, the following fungi: Fusarium spec., Such as F. acuminatum , Fusarium graminearum ( F. acuminatum ) F.asiaticum), F.avenaceum , F.crookwellense , F.culmorum , F.graminearum ( Gibberella zeae ) Fusarium (F.equiseti), Fujikura Fusarium (F.fujikoroi), fusarium (F.musarum), Fusarium oxysporum (F.oxysporum), and then incubated for Fusarium (F.proliferatum), pear Fusarium (F.poae), (F.pseudograminearum), elderberry Fusarium (F.sambucinum), cane Fusarium (F.scirpi ), Fusarium semitectum (F.semitectum) strain, Fusarium solani (F. solani), Fusarium intended Cladosporium (F.sporotrichoides), F.langsethiae, gum Fusarium (F.subglutinans), Fusarium three lines ( F.tricinctum), Fusarium moniliforme (F.verticillioides), and by a curved sp (Aspergillus spec.) produced by, for example, yellow aspergillus (A.flavus), parasitic aspergillosis (A.parasiticus), red ribbon aspergillosis ( A.nomius ), Aspergillus ( A.ochraceus ), Aspergillus ( A.clavatus ), Aspergillus ( A.terreus ), Aspergillus versicolor ( A.versicolor ), Penicillium spec. .), For example, P. verrucosum , P. viridicatum , P. citrinum, P. expansum , P. claviforme , P. claviforme (P.roqueforti), sp ergot (Claviceps spec.), for example, purple ergot fungus (C.purpurea), Clostridium ergot fungus (C.fusiformis), paspalum wheat Bacteria (C.paspali), Africa ergot fungus (C.africana), Stachybotrys species (Stachybotrys spec.) And others.

物料保護Material protection

本發明之化合物和組成物亦可用於物料保護，供保護工業物料對植物病原性真菌之攻擊及破壞。 The compounds and compositions of the present invention can also be used for material protection for protecting industrial materials from attack and destruction by phytopathogenic fungi.

此外，本發明之化合物和組成物可單獨或與其他的活性成份組合，用作為抗污組成物。 In addition, the compounds and compositions of the present invention can be used alone or in combination with other active ingredients as antifouling compositions.

在本發明內文中，工業物料應了解係指經製備用於工業上之無生命物質。例如，可受保護免於微生物變化或破壞之工業物料可為黏著劑、膠料、紙、壁紙和板子/紙板、紡織品、地毯、皮革、木材、纖維和紙巾、漆和塑膠物品、冷卻潤滑劑和其他可被微生物感染或破壞之物質。在可受保護的物料範圍內亦可提及生產工廠和建築物的部分，例如可受微生物增生作用危害之冷卻水迴路、冷卻及加熱系統及通風和空調元件。本發明範圍內之工業物料較佳地係包括黏著劑、膠料、紙及板子、皮革、木材、漆、冷卻潤滑劑及熱傳導液，更佳地木材。 In the context of the present invention, industrial materials are understood to mean inanimate substances which have been prepared for industrial use. For example, industrial materials that can be protected from microbial changes or damage can be adhesives, glues, paper, wallpaper, and boards / cardboard, textiles, carpets, leather, wood, fibers and paper towels, paint and plastic items, cooling lubricants And other substances that can be infected or destroyed by microorganisms. Within the scope of materials that can be protected, parts of production plants and buildings can also be mentioned, such as cooling water circuits, cooling and heating systems, and ventilation and air-conditioning elements that can be compromised by microbial proliferation. Industrial materials within the scope of the present invention preferably include adhesives, glues, paper and boards, leather, wood, lacquers, cooling lubricants, and thermally conductive fluids, and more preferably wood.

本發明之化合物和組成物可防阻不利的效應例如腐壞、衰敗、變色、褪色或發黴。 The compounds and compositions of the present invention prevent adverse effects such as decay, decay, discoloration, discoloration or mold.

就木材處理之情況，本發明化合物和組成物亦可用於對抗易於生長在木料上或內部的真菌。 In the case of wood treatment, the compounds and compositions of the present invention can also be used against fungi that tend to grow on or inside the wood.

術語木料(timber)係指所有類型之木材物類，及所有類型之意欲用於建築的木材加工，例如實木、高密度木材、層壓木材和合板。此外，本發明之化合物和組成物可用於保護與海水或鹹水接觸之標的物，特別是船身、篩子、網子、建築物、防波堤和通訊元件，避免附著物。 The term timber (Timber) means all types of species of wood, and all types of wood processing intended for construction, for example solid wood, high-density wood, laminated wood, and plywood. In addition, the compounds and compositions of the present invention can be used to protect objects in contact with seawater or salt water, especially hulls, sieves, nets, buildings, breakwaters and communication elements to avoid attachments.

本發明之化合物和組成物亦可用於保護儲存物品。儲存物品應了解係指植物或動物來源之天然物質或其加工製品，且就其長期的保護為所希望的。植物來源之儲存物品，例如植株或植株部位例如莖、葉、塊莖、種子、果實、榖粒可在剛收穫時或經(預)乾燥、濕化、分割、磨粉、打壓或烘烤處理後施予保護。儲存物品亦可包括未加工的木料例如建築木料、電線桿和柵欄，或成品形式之木料例如傢俱。動物來源之儲存物品有，例如生皮、皮革、羽毛和毛髮。本發明之化合物和組成物可防阻不利的效應例如腐壞、衰敗、變色、褪色或發黴。 The compounds and compositions of the present invention can also be used to protect stored items. Storage items should be understood to mean natural materials of plant or animal origin or processed products thereof, and are desirable for their long-term protection. Plant-derived storage items, such as plants or plant parts such as stems, leaves, tubers, seeds, fruits, pupae, can be just after harvest or after (pre-) drying, humidifying, dividing, milling, pressing or baking Give protection. Storage items may also include unprocessed timber such as construction timber, utility poles and fences, or timber in the form of finished products such as furniture. Storage items of animal origin include, for example, hides, leather, feathers, and hair. The compounds and compositions of the present invention prevent adverse effects such as decay, decay, discoloration, discoloration or mold.

能降解或改變工業物料之微生物包括，例如細菌、真菌、酵母菌、藻類和黏液生物。本發明之化合物和組成物較佳地係用於對抗真菌，特別是黴菌，木材-變色和木材-破壞真菌(子囊菌(Ascomycetes)、擔子菌(Basidiomycetes)、不完全菌(Deuteromycetes)和接合菌(Zygomycetes))，及對抗黏液生物和藻類。實例包括下列各屬之微生物：鏈格菌(Alternaria)，例如細鏈格菌(Alternaria tenuis)；麴菌(Aspergillus)，例如黑麴菌(Aspergillus niger)；毛殼菌(Chaetomium)，例如球毛殼菌(Chaetomium globosum)；粉孢革菌(Coniophora)，例如凹痕粉孢革菌(Coniophora puetana)；香菇(Lentinus)，例如虎皮香菇(Lentinus tigrinus)；青黴菌(Penicillium)，例如灰綠青黴菌(Penicillium glaucum)；多孔菌(Polyporus)，例如彩絨革蓋菌(Polyporus versicolor)；短梗黴(Aureobasidium)，例如出芽短梗黴(Aureobasidium pullulans)；核莖點菌(Sclerophoma)，例如松落葉病菌(Sclerophoma pityophila)；木黴菌(Trichoderma)，例如綠色木黴(Trichoderma viride)；線嘴殼屬(Ophiostoma spp.)、長味殼菌屬(Ceratocystis spp.)、腐質黴屬(Humicola spp.)、彼得殼屬(Petriella spp.)、毛束黴屬(Trichurus spp.)；革蓋菌屬(Coriolus spp.)、黏褶菌屬(Gloeophyllum spp.)、側耳屬(Pleurotus spp.)、臥孔菌屬(Poria spp.)、幹朽菌屬(Serpula spp.)和乾酪菌屬(Tyromyces spp.)、枝抱屬(Cladosporium spp.)、擬青黴菌屬(Paecilomyces spp.)、毛黴屬(Mucor spp.)，桿菌屬(Escherichia)，例如大腸桿菌(Escherichia coli)；假單胞菌(Pseudomonas)，例如銅綠假單胞菌(Pseudomonas aeruginosa)；葡萄球菌 (Staphylococcus)，例如金黃色葡萄球菌(Staphylococcus aureus)，念珠菌屬(Candida spp)及酵母屬(Saccharomyces spp)，例如釀酒酵母(Saccharomyces cerevisae)。 Microorganisms that can degrade or alter industrial materials include, for example, bacteria, fungi, yeasts, algae and slime organisms. Compounds and compositions of the present invention are preferably used against based fungi, in particular molds, wood - and wood discoloration --destroying fungi (ascomycetes (Ascomycetes), Basidiomycetes (Basidiomycetes), incomplete fungi (, Deuteromycetes) and zygomycete ( Zygomycetes )), and fight against slime organisms and algae. Examples include microorganisms of the following genera: Alternaria , such as Alternaria tenuis ; Aspergillus , such as Aspergillus niger ; Chaetomium , such as cocci Chaetomium globosum ; Coniophora , such as Coniophora puetana ; Lentinus , such as Lentinus tigrinus ; Penicillium , such as gray-green Penicillium glaucum ; Polyporus , such as Polyporus versicolor ; Aureobasidium , such as Aureobasidium pullulans ; Sclerophoma , such as pine leaves bacteria (Sclerophoma pityophila); Trichoderma (Trichoderma), for example, Trichoderma viride (Trichoderma viride); (. Ophiostoma spp) (. Ceratocystis spp) belongs to the nozzle housing, long flavor shell genus Humicola (Humicola spp), the genus Peter shell (Petriella spp), Rhizopus tufts (Trichurus spp);... .. the genus Coriolus (Coriolus spp), the genus sticky pleats (Gloeophyllum spp), Pleurotus (Pleurotus spp.), The genus Poria (Poria spp.), The genus dry rot (Serpula spp.), And the genus cheese (Tyromyces spp.), Hold the genus branch (Cladosporium spp.), The genus Paecilomyces (Paecilomyces spp), Mucor (Mucor spp), Bacillus (Escherichia), such as E. coli (Escherichia coli);.. Pseudomonas (Pseudomonas), for example, Pseudomonas aeruginosa (Pseudomonas aeruginosa); Staphylococcus (Staphylococcus ), Such as Staphylococcus aureus , Candida spp, and Saccharomyces spp, such as Saccharomyces cerevisae .

種子處理Seed treatment

本發明之化合物和組成物亦可用於保護種子避免有害的微生物，例如植物病原性微生物，如植物病原性真菌或植物病原性卵菌。術語種子如文中所用係包括休眠種子、滲調種子、預發芽種子和帶有長出根和葉之種子。 The compounds and compositions of the present invention can also be used to protect seeds from harmful microorganisms, such as phytopathogenic microorganisms, such as phytopathogenic fungi or phytopathogenic oomycetes. The term seed as used herein includes dormant seeds, osmotic seeds, pre-germinated seeds, and seeds with roots and leaves.

因此，本發明亦關於用於供保護種子避免不欲的微生物之方法，其係包括以本發明化合物或組成物處理種子之步驟。 Therefore, the present invention also relates to a method for protecting seeds from unwanted microorganisms, which comprises the step of treating seeds with a compound or composition of the present invention.

以本發明化合物或組成物處理種子係保護種子避免植物病原性微生物，亦保護出芽的種子，出芽苗株和從處理過的種子出芽後的植株。因此，本發明亦關於保護種子、發芽中的種子和出芽苗株之方法。 Treating the seed system with the compound or composition of the present invention protects the seed from phytopathogenic microorganisms, and also protects the germinated seed, the germinated seedling and the germinated plant from the treated seed. Therefore, the present invention also relates to a method for protecting seeds, germinating seeds, and germinating seedlings.

種子處理可在播種前、播種時或在播種後立即進行。 Seed treatment can be performed before, during, or immediately after sowing.

當種子處理係在播種前進行時(例如所謂的種子上施用)，種子處理可如下進行：可將種子與所欲之量的本發明化合物或組成物置入混拌器中，混拌種子與本發明化合物或組成物直到達到均勻分布在種子上。若適當，然後可將種子乾燥。 When the seed treatment is performed before sowing (for example, so-called seed application), the seed treatment can be performed as follows: The seed and the desired amount of the compound or composition of the present invention can be placed in a mixer, and the seed and the present compound are mixed. Invent the compound or composition until uniform distribution over the seeds is achieved. If appropriate, the seeds can then be dried.

本發明亦關於以本發明化合物或組成物塗覆種子。 The invention also relates to coating seeds with a compound or composition of the invention.

較佳地，係以其中夠穩定使其在處理期間無傷害發生之狀態來處理種子。一般而言，種子可在介於採收至播種後之間的任何時間來處理。通常係使用已從植株分離並去除果實之穗軸、殼、梗、外皮、毛鬚或果肉之種子。例如，可使用已採收、清潔及乾燥至溼度低於15%重量比之種子。另一種選擇，亦可使用乾燥後，例如經水處理及然後再乾燥之種子或滲調後的種子或儲存於滲調狀況的種子或預發芽種子或播種在育苗盤、育苗帶或育苗紙上的種子。 Preferably, the seed is treated in a state where it is stable enough to prevent harm from occurring during the treatment. In general, seeds can be processed at any time between harvest and sowing. Commonly used are the cobs, husks, stalks, husks, hairs, or pulp from which the fruit has been isolated and removed. For example, seeds that have been harvested, cleaned and dried to a humidity of less than 15% by weight can be used. Alternatively, after drying, for example, water-treated and then dried seeds or osmotic seeds or seeds stored in osmotic conditions or pre-germinated seeds or seeded on seedling trays, nursery belts or seedling paper seed.

施用於種子上的本發明化合物或組成物之量典型地係對種子之發芽不會有不利影響，或對生成的植物無害。此項在本發明化合物於特定 的施用率時可能具有植物毒性效應之情況下須特別謹記在心。當在決定施用於種子的本發明化合物或組成物之量時，基因轉殖植物固有的表型亦應列入考量。以便以最小的化合物使用量達到最佳的種子和出芽植物保護。 The amount of the compound or composition of the present invention applied to the seed is typically such that it does not adversely affect the germination of the seed or is not harmful to the resulting plants. This must be kept in mind in cases where the compounds of the invention may have phytotoxic effects at specific application rates. When determining the amount of a compound or composition of the invention to be applied to seeds, the phenotype inherent to the transgenic plant should also be considered. In order to achieve the best seed and sprouting plant protection with the minimum amount of compound used.

本發明化合物可，例如直接施用於種子，亦即無使用任何其他的組份且未經稀釋。本發明之化合物和組成物亦可施用於種子。 The compounds according to the invention can, for example, be applied directly to the seeds, ie without using any other components and without dilution. The compounds and compositions of the present invention can also be applied to seeds.

本發明之化合物和組成物適合用於保護任何植物種類之種子。較佳的種子為榖類(例如小麥、大麥、黑麥、小米、黑小麥和燕麥)、油菜、玉米、棉花、大豆、稻米、馬鈴薯、向日葵、菜豆、咖啡、豌豆、甜菜(例如糖用甜菜和飼料甜菜)、花生、蔬菜(例如番茄、黃瓜、洋蔥和萵苣)、草皮和觀賞植物之種子。更佳的小麥、大豆、油菜、玉米和稻米之種子。 The compounds and compositions of the present invention are suitable for protecting seeds of any plant species. Preferred seeds are millet (e.g. wheat, barley, rye, millet, triticale and oat), rapeseed, corn, cotton, soybeans, rice, potatoes, sunflower, kidney beans, coffee, peas, beets (e.g. sugar beet And fodder beets), peanuts, vegetables (such as tomatoes, cucumbers, onions and lettuce), turf and ornamental plant seeds. Better wheat, soybean, rapeseed, corn and rice seeds.

本發明之化合物和組成物可用於處理基因轉殖種子，特言之，能表現用於對抗害蟲、殺蟲劑傷害或非生物逆境之多肽或蛋白，藉此增加保護效用之植物種子。能表現用於對抗害蟲、殺蟲劑傷害或非生物逆境之多肽或蛋白之植物種子可含有至少一種得以表現該多肽或蛋白之異源基因。這些基因轉植種子中的異源基因可源自於，例如芽孢桿菌(Bacillus)、根瘤菌(Rhizobium)、假單胞菌(Pseudomonas)、沙雷菌(Serratia)、木黴菌(Trichoderma)、棒形桿菌(Clavibacter)、繡球菌(Glomus)或黏帚黴菌(Gliocladium)屬的微生物。這些異源基因較佳地係源自芽孢桿菌屬，在該情況下此基因產物係有效對抗歐洲玉米螟和西方玉米根蟲。特佳地，異源基因係源自蘇雲金芽孢桿菌。 The compounds and compositions of the present invention can be used to treat genetically modified seeds, in particular, they can express plant or plant seeds that are resistant to pests, pesticide damage, or abiotic stresses, thereby increasing the protective effect. Plant seeds capable of expressing a polypeptide or protein used to combat pests, pesticide damage or abiotic stress may contain at least one heterologous gene capable of expressing the polypeptide or protein. The heterologous genes in these gene-transplanted seeds can be derived from, for example, Bacillus, Rhizobium, Pseudomonas, Serratia, Trichoderma, Stick Microorganisms of the genus Clavibacter, Glomus or Gliocladium. These heterologous genes are preferably derived from Bacillus, in which case the gene product is effective against European corn borer and Western corn rootworm. Particularly preferably, the heterologous gene line is derived from Bacillus thuringiensis.

抗黴效應Antifungal effect

本發明之化合物和組成物亦可具有非常良好的抗黴效應。其具有非常廣效的抗黴活性，特別是對抗皮癬菌(dermatophytes)和酵母菌、黴菌和雙相真菌(例如對抗念珠菌屬(Candida)，如白色念珠菌(Candida albicans)、光滑念珠菌(Candida glabrata))，及絮狀表皮癬菌(Epidermophyton floccosum)，麯菌屬(Aspergillus)例如黑麯菌(Aspergillus niger)和煙麯菌(Aspergillus fumigatus)，毛癬菌屬(Trichophyton)例如須癬毛癬菌(Trichophyton mentagrophytes)，小孢癬菌屬(Microsporon species)例如犬小孢 癬菌(Microsporon canis)和奧杜盤小孢癬菌(audouinii)。列舉這些真菌並非限制所涵蓋的黴菌範圍，而僅是說明特徵。 The compounds and compositions of the present invention can also have very good anti-mildew effects. It has very broad antifungal activity, especially against dermatophytes and yeasts, molds and biphasic fungi (e.g. against Candida, such as Candida albicans, Candida glabrata) (Candida glabrata)), and Epidermophyton floccosum, Aspergillus such as Aspergillus niger and Aspergillus fumigatus, Trichophyton such as trichophyton Trichophyton mentagrophytes, Microsporon species such as Microsporon canis and audouinii. The enumeration of these fungi is not a limitation of the range of molds covered, but merely characterization.

本發明之化合物和組成物亦可用於魚類和甲殼類養殖中防治重要的真菌病原，例如鱒魚中的異絲水黴菌(saprolegnia diclina)和螯蝦中的寄生水黴菌(saprolegnia parasitica)。 The compounds and compositions of the present invention can also be used to control important fungal pathogens in fish and crustacean farming, such as saprolegnia diclina in trout and saprolegnia parasitica in crawfish.

本發明之化合物和組成物因此可用於醫療和非醫療應用。 The compounds and compositions of the present invention are therefore useful in medical and non-medical applications.

植物生長調節Plant growth regulation

本發明之化合物和組成物亦可，以特別的濃度或施用率，用作為除草劑、安全劑、生長調節劑或植物性質改良劑或做為殺微生物劑，例如作為殺細菌劑、殺病毒劑(包括抗類病毒之組成物)或作為抗MLO(類黴漿菌體)和RLO(類立克次體)之組成物。 The compounds and compositions of the present invention can also be used as herbicides, safeners, growth regulators or plant property modifiers or as microbicides at specific concentrations or application rates, such as bactericides, virus killers (Including antiviral composition) or as a composition against MLO (mycoplasma-like body) and RLO (rickettsia-like body).

本發明之化合物和組成物可介入植物的生理過程且因此亦可用作為植物生長調節劑。植物生長調節劑可對植物施加各種效應。物質之效應基本上係依照相對於植物發育階段的施用時間，及依照施用於植物或其環境的活性成份之量以及依照施用的種類而定。在各情況下，生長調節劑對於作物植株應具有特定的所欲效應。 The compounds and compositions of the present invention can be involved in the physiological processes of plants and can therefore also be used as plant growth regulators. Plant growth regulators can exert various effects on plants. The effect of the substance basically depends on the time of application relative to the stage of plant development, and on the amount of active ingredient applied to the plant or its environment, and on the type of application. In each case, the growth regulator should have a specific desired effect on the crop plant.

生長調節效應，包括包括早期萌芽、較佳的發育、更發達的根系及/或提升的根生長、增加的分蘗能力、更多產的分蘗、早開花、增加植物高度及/或生物質、矮化莖、提升芽生長、核/穗的數目、穗/m2之數目、匍匐枝數目及/或花數目、增進採收指數、較大葉片、較少死亡的基葉、提升葉序、較早成熟/早期熟果、同時成熟、增加穀粒飽實、較佳的熟果、較大的果實/蔬菜大小、發芽抗性及降低伏倒。 Growth-regulating effects , including early germination, better development, more developed root systems and / or enhanced root growth, increased tillering capacity, more productive tillers, early flowering, increased plant height and / or biomass, short Stem, increase bud growth, number of nuclei / ears, number of ears / m 2 , number of twigs and / or flowers, increase harvest index, larger leaves, less dead base leaves, increase leaf order, more Early maturity / early ripe fruit, simultaneous maturity, increased grain fullness, better ripe fruit, larger fruit / vegetable size, germination resistance and reduced lodging.

增加或提升產量，係指每公頃的總生物質，每公頃的產量，核/果實重量、種子大小及/或公石重量以及增加的產物量，其包括：提升與大小分布有關的可操作性(例如核仁、果實)、同時成熟、榖粒水份、較佳研磨、較佳葡萄酒釀造、較佳酒釀造、增加果汁產量、收成量、消化性、沉降值、降落數、莢穩定性、儲存穩定性、改善纖維長度/強度/一致性、增加乳量及/或符合青貯飼料動物之品質、適合烹調及油炸； 提升與下列有關的可銷售性：提升果實/榖粒品質、大小分布(例如核仁、果實)、增加儲存/保存期限、緊實度/柔軟度、口味(氣味、質地等)、等級(例如大小、形狀、莓果數目)、每束之莓果/果實數目、脆度、新鮮度、覆蓋蠟、生理病症之頻率、顏色；增加所欲的成份，例如蛋白質含量、脂肪酸、油含量、油品質、胺基酸組成、糖含量、酸含量(pH)、糖/酸比(Brix)、多酚、澱粉含量、營養品質、麩質含量/指數、能量、口味；降低不欲的成份，例如較低的黴菌毒素、較低的黃麴毒素、土腥味、酚系氣味、漆酶、多酚氧化酶和過氧化酶、硝酸鹽含量。 Increasing or increasing yield refers to total biomass per hectare, yield per hectare, kernel / fruit weight, seed size and / or stone weight, and increased product volume, including: increasing operability related to size distribution (E.g. kernels, fruits), simultaneous maturity, water content in caraway, better grinding, better winemaking, better winemaking, increased juice yield, yield, digestibility, sedimentation value, drop count, pod stability, Storage stability, improved fiber length / strength / consistency, increased milk volume and / or quality of silage animals, suitable for cooking and frying; improved saleability in relation to: improved fruit / pellet quality, size distribution (E.g. kernels, fruits), increase storage / storage period, firmness / softness, taste (smell, texture, etc.), grade (e.g. size, shape, number of berries), number of berries / fruit per bunch, Crispness, freshness, covering wax, frequency and color of physiological disorders; increase desired ingredients, such as protein content, fatty acids, oil content, oil quality, amino acid composition, sugar content, acid content (pH), Sugar / acid ratio (Brix), polyphenols, starch content, nutritional quality, gluten content / index, energy, taste; reduce unwanted ingredients, such as lower mycotoxins, lower baical toxins, and earthy smell , Phenolic odor, laccase, polyphenol oxidase and peroxidase, nitrate content.

植物生長調節化合物可用於，例如，延緩植物的營養生長。此生長抑制為經濟上有利的，例如就雜草的情況下，因為其可能因此降低觀賞庭園、公園和運動設施中，路旁、機場或果園之割草頻率。抑制路旁和管路附近或電纜上方，或一般其中繁茂植物生長為不欲的區域中之草本和木本植物生長，亦為重要的。 Plant growth regulating compounds can be used, for example, to retard the vegetative growth of plants. This growth inhibition is economically advantageous, for example in the case of weeds, as it may therefore reduce the frequency of mowing in ornamental gardens, parks and sports facilities, roadsides, airports or orchards. It is also important to inhibit the growth of herbs and woody plants in roadsides and near pipelines or above cables, or generally in areas where lush vegetation grows into unwanted areas.

使用植物調節劑來抑制穀類之縱向生長亦為重要的。此項係降低或完全消除收割前植物之伏倒風險。此外，在穀類的情況下，生長調節劑可強化莖稈，其亦抵抗伏倒。應用生長調節劑縮短和強化莖稈，而得以在無任何穀類作物伏倒之風險下，將較高的肥料量有效利用於增加產量。 It is also important to use plant regulators to inhibit the vertical growth of cereals. This item reduces or completely eliminates the risk of plants falling down before harvesting. In addition, in the case of cereals, the growth regulator can strengthen the stalk, which also resists lodging. The use of growth regulators shortens and strengthens the stalks, so that a higher amount of fertilizer can be effectively used to increase yield without the risk of any cereal crops falling down.

在許多作物植物中，抑制營養生長而得以密植，且其因此可能在以土壤表面為基礎下達到較高的產量。以此法得到的較小植株之另外的好處為作物較容易栽培和採收。 In many crop plants, vegetative growth is suppressed for dense planting, and thus it is possible to reach higher yields based on the soil surface. Another advantage of the smaller plants obtained this way is that the crops are easier to grow and harvest.

降低營養植物生長亦可導致增加或提高產量，因為比起植物的營養部位，營養和吸收更有利於花和果實形成。 Decreasing vegetative plant growth can also lead to increased or increased yield, as nutrients and absorption are more conducive to flower and fruit formation than the vegetative parts of the plant.

或者，生長調節劑亦可用於促進營養生長。當採收的為營養性植物部位時此項大為有利。然而，促進營養性生長亦可促進其中更多吸收所形成之營養性生長，造成更多或更大的果實。 Alternatively, growth regulators can also be used to promote vegetative growth. This is particularly advantageous when harvested from vegetative plant parts. However, promoting vegetative growth can also promote vegetative growth formed by more absorption thereof, resulting in more or larger fruits.

再者，對於生長或產量之有利的效應可經由提升營養素使用效率來達成，特別是氮(N)-使用效率、磷(P)-使用效率、水使用效率、改善蒸散率、呼吸率及/或CO2同化率、較佳的結瘤作用、改善Ca-代謝作用。 Moreover, beneficial effects on growth or yield can be achieved by increasing nutrient use efficiency, especially nitrogen (N) -use efficiency, phosphorus (P) -use efficiency, water use efficiency, improved evapotranspiration, respiration rate and / Or CO 2 assimilation rate, better nodulation, and improved Ca-metabolism.

同樣的，生長調節劑可用於改變植物之組成，其轉而可造成採收產物之品質提升。在生長調節劑的影響下，可形成單性果實。此外，其可能影響花的性別。其亦可能產生不育性花粉，其對於雜交種子之選育和生產大為重要。 Similarly, growth regulators can be used to alter the composition of plants, which in turn can lead to improved quality of harvested products. Under the influence of growth regulators, parthenocarpic fruits can be formed. In addition, it may affect the sex of the flower. It may also produce sterile pollen, which is very important for the selection and production of hybrid seeds.

使用生長調節劑可控制植物的分枝。在一方面，藉由破壞頂端優勢，可能促進側芽的發育，其特別是在觀賞植物之培養，及在結合抑制生長上可能非常可取的。在另一方面，然而，亦可能抑制側芽的生長。此效應，例如在菸草培養上或番茄的培養上為特別有利的。 The use of growth regulators can control the branching of plants. On the one hand, by destroying the apical dominance, it is possible to promote the development of lateral buds, which may be particularly desirable in the cultivation of ornamental plants, and in combination to inhibit growth. On the other hand, however, it is also possible to inhibit the growth of lateral buds. This effect is particularly advantageous, for example, in tobacco culture or tomato culture.

在生長調節劑的影響下，可控制植物葉子的量，使得在所欲的時間進行植株之落葉。此等落葉作用在機械採收棉花上扮演著重要角色，但對於幫助其他作物收穫上，例如葡萄栽培上亦為有利的。亦可進行植物之落葉用以降低其在轉植前植株的蒸散作用。 Under the influence of the growth regulator, the amount of plant leaves can be controlled so that the leaves of the plant can be deciduous at a desired time. These deciduous effects play an important role in mechanically harvesting cotton, but they are also beneficial in helping other crops to be harvested, such as viticulture. Defoliation of the plant can also be performed to reduce its evapotranspiration before planting.

再者，生長調節劑可調節植物老化，其可造成較長的植物之綠葉著色期，較長的榖粒充實期，提高產量品質。 Furthermore, the growth regulator can regulate the aging of plants, which can cause a longer green leaf coloring period of plants, a longer flesh filling period, and improve yield and quality.

生長調節劑同樣地可用於調節裂果。在一方面，其可防止早熟性裂果。在另一方面，其亦可促進裂果或甚至花朵敗育，以達到所欲的量(「疏化」)。此外，可在採收時使用生長調節劑用以降低需要摘離果實的力道，以便於得以進行機器採收或幫助人工採收。 Growth regulators can also be used to regulate split fruit. In one aspect, it prevents premature cracking. On the other hand, it can also promote split fruit or even flower abortion to reach the desired amount ("thinning"). In addition, growth regulators can be used during harvesting to reduce the force required to remove the fruit, so as to facilitate machine harvesting or assist manual harvesting.

生長調節劑亦可於採收之前或之後用於達到加快或另外延遲採收物質之成熟。當在最適化調整市場需求時，此項特別有利。再者，生長調節劑在某些情況下可改善果實顏色。此外，生長調節劑亦可用於特定的時期內同步成熟。此項係建立以單一操作完全機械或人工採收之先決條件，例如就菸草、番茄或咖啡的情況而言。 Growth regulators can also be used to achieve accelerated or otherwise delayed maturity of the harvested material before or after harvesting. This is particularly advantageous when adjusting market demand for optimization. Furthermore, growth regulators can improve fruit color in some cases. In addition, growth regulators can also be used to synchronize maturity during specific periods. This item establishes the prerequisites for complete mechanical or manual harvesting in a single operation, such as in the case of tobacco, tomato or coffee.

藉由使用生長調節劑，其另外可能影響種子的休眠或植物發芽，使得例如鳳梨或苗圃的觀賞植物，例如於其正常上無此傾向之時間萌 芽、發芽或開花。在有霜害風險之區域中，可能希望在生長調節劑的幫助下延遲種子之發芽或萌芽，以便於避免由晚霜所造成的損害。 By using a growth regulator, it may additionally affect the dormancy of the seed or plant germination, such that an ornamental plant such as ananas or nursery, for example, germinates, germinates, or blooms at a time when it normally does not have this tendency. In areas at risk of frost damage, it may be desirable to delay the germination or germination of seeds with the help of growth regulators in order to avoid damage caused by late frost.

最後，生長調節劑可引發植物對於霜、乾旱或高鹽度土壤的抗性。此項讓一般不適合此目的之區域得以培養植物。 Finally, growth regulators can trigger plant resistance to frost, drought, or high-salinity soils. This allows plants to be grown in areas that are generally not suitable for this purpose.

植物防禦調節劑Plant Defense Regulator

本發明之化合物和組成物亦具有植物之有力的強化效應。因此，其可用於帶動植物之防禦力對抗不欲的微生物攻擊。 The compounds and compositions of the present invention also have potent strengthening effects in plants. Therefore, it can be used to drive the defense of plants against unwanted microbial attacks.

植物強化(抗性-引發)物質在本文中為能刺激植物防禦系統之物質，使經處理過的植物，當隨後接種不欲的微生物時，能對這些不欲的微生物展現高度的抗性。 Plant fortification (resistance-priming) substances herein are substances that can stimulate the plant defense system, so that treated plants, when subsequently inoculated with unwanted microorganisms, can exhibit a high degree of resistance to these unwanted microorganisms.

另外，在本發明內文中，植物生理效應係包括下列： 非生物耐逆性，包括對高溫或低溫的耐受性、乾旱耐受性和乾旱脅迫後之復原、水使用效能(與降低水消耗有關)、水災耐受性、臭氧逆境和UV耐受性、對化學品如重金屬、鹽類、殺蟲劑之耐受性。 In addition, in the context of the present invention, the physiological effects of plants include the following: Abiotic stress tolerance, including tolerance to high or low temperature, drought tolerance and recovery after drought stress, water use efficiency (and reduction of water consumption) (Relevant), flood tolerance, ozone stress and UV resistance, resistance to chemicals such as heavy metals, salts, pesticides.

生物耐逆性，包括增加的真菌抗性和增加的抗線蟲、病毒和細菌之抗性。在本發明內文中，生物耐逆性較佳地係包括增加的真菌抗性和增加的抗線蟲和細菌之抗性。 Biological stress resistance, including increased fungal resistance and increased resistance to nematodes, viruses and bacteria. In the context of the present invention, biological stress tolerance preferably includes increased fungal resistance and increased resistance to nematodes and bacteria.

增加的植物活力，包括植物健康/植物品質和種子活力，降低伏倒、改善外觀、增加逆境期之後的復原性、改善色素沉著(例如葉綠素含量、持綠效應)和改善光合作用效能。 Increased plant vitality, including plant health / plant quality and seed vitality, reduced lodging, improved appearance, increased resilience after periods of stress, improved pigmentation (eg, chlorophyll content, green-holding effect), and improved photosynthetic performance.

施用Apply

本發明化合物可直接或例如以即用溶液、乳劑、水基和油基懸浮劑、粉劑、可濕性粉劑、糊劑、可溶性粉劑、粉塵劑、可溶性粒劑、佈施用之粒劑、濃縮懸浮乳劑、注入本發明化合物之天然產品、注入本發明化合物之合成產品、肥料以及微膠囊化於聚合物中之形式來施用。 The compounds of the present invention can be used directly or, for example, as ready-to-use solutions, emulsions, water-based and oil-based suspensions, powders, wettable powders, pastes, soluble powders, dusts, soluble granules, cloth-applied granules, concentrated suspensions Emulsions, natural products infused with compounds of the invention, synthetic products infused with compounds of the invention, fertilizers, and microencapsulated polymers are applied.

施用係以習用的方式，例如以浸泡、噴灑、噴霧、撒播、撒粉、泡沫、散佈其上等等來進行。亦可藉由超低容量法，經由滴灌系統或淋灌 施用佈署本發明化合物，將其施用於犁溝或注射至土壤莖或枝幹。另外亦可藉由敷片、漆或其他敷料來施用本發明化合物。 Application is carried out in a customary manner, for example by soaking, spraying, spraying, spreading, dusting, foaming, spreading on, and the like. The compound of the present invention can also be applied by drip irrigation system or drip irrigation by ultra-low volume method, applied to furrows or injected into soil stems or branches. Alternatively, the compounds of the present invention can be applied by a patch, lacquer or other dressing.

施用於植物、植物部位、果實、種子或土壤之本發明化合物的有效及植物相容之量將依照各種因子而定，例如所用的化合物/組成物、處理的標的物(植物、植物部位、果實、種子或土壤)、處理類型(灑粉、噴霧、拌種)、處理目的(治療性和保護性)、微生物類型、微生物的發育階段、微生物的敏感性、作物生長階段和環境狀況。 The effective and phytocompatible amount of a compound of the present invention applied to a plant, plant part, fruit, seed or soil will depend on various factors, such as the compound / composition used, the subject matter treated (plant, plant part, fruit , Seed or soil), type of treatment (sprinkling, spraying, seed dressing), purpose of treatment (therapeutic and protective), type of microorganism, stage of development of microorganism, sensitivity of microorganism, stage of crop growth and environmental conditions.

當本發明化合物係用作為殺真菌劑時，依照施用的種類，施用率可在相當廣泛的範圍內變化。就處理植物部位，例如葉片，施用率範圍可從0.1至10000g/ha，較佳地10至1000g/ha，更佳地50至300g/ha(在以噴灑或淋滴來施用的情況下，甚至可能降低施用率，特別是使用例如岩棉或真珠石之惰性物質時)。就種子處理，施用率範圍為每100kg的種子可從0.1至200g，較佳地每100kg的種子1至150g，更佳地每100kg的種子2.5至25g，甚佳地每100kg的種子2.5至12.5g。就處理土壤，施用率範圍可從0.1至10000g/ha，較佳地1至5000g/ha。 When the compound of the present invention is used as a fungicide, the application rate can be varied within a relatively wide range depending on the kind of application. For treating plant parts, such as leaves, the application rate may range from 0.1 to 10000 g / ha, preferably 10 to 1000 g / ha, more preferably 50 to 300 g / ha (in the case of application by spraying or dripping, even May reduce application rates, especially when using inert materials such as rock wool or pearlite). For seed treatment, the application rate ranges from 0.1 to 200 g per 100 kg of seeds, preferably 1 to 150 g per 100 kg of seeds, more preferably 2.5 to 25 g per 100 kg of seeds, and very preferably 2.5 to 12.5 per 100 kg of seeds. g. For treating soil, the application rate may range from 0.1 to 10,000 g / ha, preferably 1 to 5000 g / ha.

這些施用率僅為實例且不希望限制本發明之範圍。 These application rates are examples only and are not intended to limit the scope of the invention.

本發明係藉由下列實施例加以說明。然而，本發明不限於該等實施例。 The invention is illustrated by the following examples. However, the present invention is not limited to these embodiments.

製備實施例Preparation Example 製備3-[2-(1-氟環丙基)-3-(4-氯苯基)-2-羥基-丁-3-烯基]咪唑-4-甲腈(I-05)     Preparation of 3- [2- (1-fluorocyclopropyl) -3- (4-chlorophenyl) -2-hydroxy-but-3-enyl] imidazole-4-carbonitrile (I-05)    

Figure TW201945344A_D0179
Figure TW201945344A_D0179

將鎂碎屑(559mg,22.9mmol,2.5當量)先於rt(rt=室溫=21℃)氬氣下攪拌1h，然後於持續攪拌下覆蓋Et2O(3mL)和1,2-二溴甲烷(3滴)。將生成的懸浮液緩和加熱直到氣體開始逸出，然後於室溫另再攪拌20min。加入數滴的1-(1-溴乙烯基)-4-氯-苯，然後將生成的混合物冷卻至0-5℃，及將 剩餘量的1-(1-溴乙烯基)-4-氯-苯(總量：2.00g,9.19mmol)溶於Et2O(10mL)並經由注射泵浦逐滴加入(12mL/h)。添加後，將反應混合物於0-5℃攪拌1h。使用碘作為指試劑滴定所生成的溶液，得到0.20M濃度。 The magnesium crumbs (559mg, 22.9mmol, 2.5 equivalents) were stirred under argon (rt = rt = room temperature = 21 ° C) for 1h before being covered with Et 2 O (3mL) and 1,2-dibromomethane under continuous stirring. (3 drops). The resulting suspension was gently heated until the gas started to escape, and then stirred at room temperature for another 20 min. Add a few drops of 1- (1-bromovinyl) -4-chloro-benzene, then cool the resulting mixture to 0-5 ° C, and the remaining amount of 1- (1-bromovinyl) -4-chloro -Benzene (total: 2.00 g, 9.19 mmol) was dissolved in Et 2 O (10 mL) and added dropwise (12 mL / h) via a syringe pump. After the addition, the reaction mixture was stirred at 0-5 ° C for 1 h. The resulting solution was titrated using iodine as a finger reagent to obtain a concentration of 0.20M.

將得到的格任亞溶液(Grignard solution)(12mL,0.20M,2.38mmol)於5℃逐滴加到3-[2-(1-氟環丙基)-2-側氧-乙基]咪唑-4-甲腈(461mg,2.38mmol,1.0eq(eq=equiv=當量))之二氯甲烷(5mL)溶液中。將反應混合物於0-5℃另再攪拌2h，然後於0-5℃加入飽和的NH4Cl水溶液中止反應。將生成的混合物以水稀釋，然後以乙酸乙酯(3 x 20mL)萃取。將組合的有機層以食鹽水清洗，乾燥(Chem Elut)，然後於真空濃縮至乾。將油狀殘餘物藉由層析於矽膠上以正庚烷/乙酸乙酯(100：0至50：50)混合物溶離，進行純化。蒸發溶劑，得到481mg(58%)的3-[2-(1-氟環丙基)-3-(4-氯苯基)-2-羥基-丁-3-烯基]咪唑-4-甲腈為無色固體。 The obtained Grignard solution (12 mL, 0.20 M, 2.38 mmol) was added dropwise to 3- [2- (1-fluorocyclopropyl) -2-oxo-ethyl] imidazole at 5 ° C. 4-carbonitrile (461 mg, 2.38 mmol, 1.0 eq (eq = equiv = equivalent)) in dichloromethane (5 mL). The reaction mixture was stirred for another 2 h at 0-5 ° C, and then a saturated NH 4 Cl aqueous solution was added at 0-5 ° C to stop the reaction. The resulting mixture was diluted with water and then extracted with ethyl acetate (3 x 20 mL). The combined organic layers were washed with brine, dried (Chem Elut), and then concentrated to dryness in vacuo. The oily residue was purified by chromatography on silica gel with a mixture of n-heptane / ethyl acetate (100: 0 to 50:50). Evaporation of the solvent gave 481 mg (58%) of 3- [2- (1-fluorocyclopropyl) -3- (4-chlorophenyl) -2-hydroxy-but-3-enyl] imidazole-4-methyl Nitrile is a colorless solid.

MS(ESI)：332([M+H]+) MS (ESI): 332 ([M + H] + )

製備2-(1-氯環丙基)-3-(2-氟苯基)-1-[5-(三氟甲基)咪唑-1-基]丁-3-烯-2-醇(I-08)     Preparation of 2- (1-chlorocyclopropyl) -3- (2-fluorophenyl) -1- [5- (trifluoromethyl) imidazol-1-yl] but-3-en-2-ol (I -08)    

Figure TW201945344A_D0180
Figure TW201945344A_D0180

將鎂碎屑(735mg,30.2mmol,1.5equiv)先於rt氬氣下攪拌1h，然後於持續攪拌下覆蓋Et2O(10mL)和1,2-二溴甲烷(8滴)。將生成的懸浮液緩和加熱直到氣體開始逸出，然後於室溫另再攪拌20min。加入數滴的1-(1-溴乙烯基)-2-氟-苯[根據US2009/30238所製備]，然後將生成的混合物冷卻至0-5℃，及將剩餘量的1-(1-溴乙烯基)-2-氟-苯(總量：4.50g,90% GC-純度20.1mmol)溶於Et2O(40mL)並緩慢加入。添加後，將反應混合物於0-5℃攪拌1h。使用碘作為指試劑滴定所生成的溶液，得到0.26M濃度。 The magnesium crumbs (735 mg, 30.2 mmol, 1.5 equiv) were stirred under rt argon for 1 h, and then covered with Et 2 O (10 mL) and 1,2-dibromomethane (8 drops) under continuous stirring. The resulting suspension was gently heated until the gas started to escape, and then stirred at room temperature for another 20 min. Add a few drops of 1- (1-bromovinyl) -2-fluoro-benzene [prepared according to US2009 / 30238], then cool the resulting mixture to 0-5 ° C, and the remaining amount of 1- (1- Bromovinyl) -2-fluoro-benzene (total: 4.50 g, 90% GC-purity 20.1 mmol) was dissolved in Et 2 O (40 mL) and added slowly. After the addition, the reaction mixture was stirred at 0-5 ° C for 1 h. The resulting solution was titrated using iodine as a finger reagent to obtain a 0.26M concentration.

將得到的格任亞溶液(10mL,0.26M,2.60mmol,1.11eq)於5℃逐滴加到1-(1-氯環丙基)-2-[5-(三氟甲基)咪唑-1-基]乙酮(591mg,2.34mmol)之二氯甲烷(12mL)溶液中。將反應混合物於0-5℃另再攪拌2h，然後於0-5℃加入飽和的NH4Cl水溶液中止反應。將生成的混合物以水稀釋，然後以乙酸乙酯(3 x 20mL)萃取。將組合的有機層以食鹽水清洗，乾燥(Chem Elut)，然後於真空濃縮至乾。將油狀殘餘物藉由層析於矽膠上以正庚烷/乙酸乙酯(100：0至50：50)混合物溶離，進行純化。蒸發溶劑，將殘餘物進一步以HPLC純化，得到458mg(52%)的2-(1-氯環丙基)-3-(2-氟苯基)-1-[5-(三氟甲基)咪唑-1-基]丁-3-烯-2-醇為無色固體。 The resulting Grignard solution (10 mL, 0.26 M, 2.60 mmol, 1.11 eq) was added dropwise to 1- (1-chlorocyclopropyl) -2- [5- (trifluoromethyl) imidazole- 1-yl] ethanone (591 mg, 2.34 mmol) in dichloromethane (12 mL). The reaction mixture was stirred for another 2 h at 0-5 ° C, and then a saturated NH 4 Cl aqueous solution was added at 0-5 ° C to stop the reaction. The resulting mixture was diluted with water and then extracted with ethyl acetate (3 x 20 mL). The combined organic layers were washed with brine, dried (Chem Elut), and then concentrated to dryness in vacuo. The oily residue was purified by chromatography on silica gel with a mixture of n-heptane / ethyl acetate (100: 0 to 50:50). The solvent was evaporated and the residue was further purified by HPLC to give 458 mg (52%) of 2- (1-chlorocyclopropyl) -3- (2-fluorophenyl) -1- [5- (trifluoromethyl) Imidazol-1-yl] but-3-en-2-ol is a colorless solid.

MS(ESI)：375([M+H]+) MS (ESI): 375 ([M + H] + )

製備1-[2-(2,4-二氟苯基)-2-羥基-3-苯基丁-3-烯-1-基]-1H-咪唑-5-甲腈(I-07)     Preparation of 1- [2- (2,4-difluorophenyl) -2-hydroxy-3-phenylbut-3-en-1-yl] -1H-imidazole-5-carbonitrile (I-07)    

Figure TW201945344A_D0181
Figure TW201945344A_D0181

將鎂碎屑(100mg,4.10mmol,1.5當量)首先於氬氣流下以空氣槍加熱(大約150℃)攪拌10min，然後冷卻至rt。於劇烈攪拌及緩和加熱下加入Et2O(2mL)，接著1,2-二溴甲烷(2滴)，引發反應。攪拌大約1h，上清液變成混濁及灰白色。將混合物冷卻至0℃並加入2滴的(1-溴乙烯基)苯(500mg,2.73mmol,1.0當量)溶於Et2O(4mL)之溶液。攪拌10分鐘後，於劇烈攪拌維持在0℃溫度下，將全部剩餘的(1-溴乙烯基)苯之醚溶液以逐滴方式緩慢加入。添加後，將反應混合物於0-5℃另再攪拌30min。使用碘作為指試劑滴定所生成的溶液，得到0.19M濃度。 Magnesium crumbs (100 mg, 4.10 mmol, 1.5 equivalents) were first heated with an air gun (approximately 150 ° C) for 10 min under an argon stream, and then cooled to rt. Et2O (2 mL) was added with vigorous stirring and gentle heating, followed by 1,2-dibromomethane (2 drops) to initiate the reaction. After stirring for about 1 h, the supernatant turned cloudy and off-white. The mixture was cooled to 0 ° C and a solution of 2 drops of (1-bromovinyl) benzene (500 mg, 2.73 mmol, 1.0 equivalent) in Et2O (4 mL) was added. After stirring for 10 minutes, all the remaining (1-bromovinyl) benzene ether solution was added slowly in a dropwise manner while maintaining vigorous stirring at 0 ° C. After the addition, the reaction mixture was stirred for another 30 min at 0-5 ° C. The resulting solution was titrated using iodine as a finger reagent to obtain a concentration of 0.19M.

將一經烘乾的20mL微波小瓶通入氬氣及隨後裝入1-[2-(2,4-二氟苯基)-2-側氧乙基]-1H-咪唑-5-甲腈(100mg,95%純度，0.38mmol,1.0當量)，接著於氬氣壓下加入二氯甲烷(4mL)。將生成的混合物冷卻至0℃並加 入新鮮製備的格任亞溶液(2.0mL,0.19M,0.38mmol,1.0當量)。將反應於0℃攪拌1h，之後以飽和的氯化銨水溶液中止反應。將有機層分離並於減壓下蒸發溶劑。將殘餘物經由矽膠濾心(2g)過濾，以二氯甲烷溶離並分溶成二個溶離份。如LCMS判定，將含有較少未反應酮起始物之溶離份，於減壓下濃縮至乾，並以逆相製備式HPLC純化，得到70mg(51%)的1-[2-(2,4-二氟苯基)-2-羥基-3-苯基丁-3-烯-1-基]-1H-咪唑-5-甲腈。 A dried 20 mL microwave vial was purged with argon and then filled with 1- [2- (2,4-difluorophenyl) -2-oxoethyl] -1H-imidazole-5-carbonitrile (100 mg , 95% purity, 0.38 mmol, 1.0 eq.), Then dichloromethane (4 mL) was added under argon pressure. The resulting mixture was cooled to 0 ° C and a freshly prepared Grignard solution (2.0 mL, 0.19 M, 0.38 mmol, 1.0 equivalent) was added. The reaction was stirred at 0 ° C. for 1 h, and then the reaction was stopped with a saturated aqueous ammonium chloride solution. The organic layer was separated and the solvent was evaporated under reduced pressure. The residue was filtered through a silica gel filter (2 g), dissolved in dichloromethane and separated into two fractions. As judged by LCMS, the fractions containing less unreacted ketone starting material were concentrated to dryness under reduced pressure and purified by reverse-phase preparative HPLC to obtain 70 mg (51%) of 1- [2- (2, 4-difluorophenyl) -2-hydroxy-3-phenylbut-3-en-1-yl] -1H-imidazole-5-carbonitrile.

MS(ESI)：352([M+H]+) MS (ESI): 352 ([M + H] + )

製備1-(2-苯甲基-2-羥基-3-苯基丁-3-烯-1-基)-1H-咪唑-5-甲腈(I-04)     Preparation of 1- (2-benzyl-2-hydroxy-3-phenylbut-3-en-1-yl) -1H-imidazole-5-carbonitrile (I-04)    

Figure TW201945344A_D0182
Figure TW201945344A_D0182

將鎂碎屑(200mg,8.20mmol,1.5當量)於氬氣下密封於微波試管中並加入Et2O(2mL)，接著1,2-二溴甲烷(2滴)及於rt攪拌20min。加入2滴的(1-溴乙烯基)苯(1.00g,5.46mmol,1.0當量s)溶於Et2O(5mL)之溶液。攪拌10分鐘後，將混合物冷卻至0℃及於劇烈攪拌，維持在0℃溫度下，以逐滴方式將全部剩餘的(1-溴乙烯基)苯之醚溶液緩慢加入。添加後，將反應混合物於0-5℃另攪拌15min。使用碘作為指試劑滴定所生成的溶液，得到0.30M濃度。 The magnesium crumbs (200 mg, 8.20 mmol, 1.5 equivalents) were sealed in a microwave test tube under argon and Et2O (2 mL) was added, followed by 1,2-dibromomethane (2 drops) and stirred at rt for 20 min. A solution of 2 drops of (1-bromovinyl) benzene (1.00 g, 5.46 mmol, 1.0 equivalent s) in Et2O (5 mL) was added. After stirring for 10 minutes, the mixture was cooled to 0 ° C and stirred vigorously, maintaining the temperature at 0 ° C, and the entire remaining (1-bromovinyl) benzene ether solution was slowly added dropwise. After the addition, the reaction mixture was stirred for another 15 min at 0-5 ° C. The resulting solution was titrated using iodine as a finger reagent to obtain a concentration of 0.30M.

於氬氣壓下，將一密封試管裝入1-(2-側氧-3-苯基丙基)-1H-咪唑-5-甲腈(200mg,0.89mmol,1.0當量)之二氯甲烷(3mL)溶液。將生成的混合物冷卻至0℃並加入新鮮製備的格任亞溶液(3.08mL,0.30M,0.93mmol,1.05當量)。將反應於0℃攪拌2h，之後以飽和的氯化銨水溶液中止反應。將生成的混合物以乙酸乙酯稀釋並以Chem Elut過濾，以另外的乙酸乙酯沖洗。於減壓下從濾液蒸發溶劑，並將殘餘物以製備式HPLC純化，得到23mg(7%)的1-(2-苯甲基-2-羥基-3-苯基丁-3-烯-1-基)-1H-咪唑-5-甲腈。 Under a argon pressure, a sealed test tube was charged with 1- (2-lanthoxy-3-phenylpropyl) -1H-imidazole-5-carbonitrile (200 mg, 0.89 mmol, 1.0 equivalent) in dichloromethane (3 mL). ) Solution. The resulting mixture was cooled to 0 ° C and a freshly prepared Grignard solution (3.08 mL, 0.30M, 0.93 mmol, 1.05 equivalent) was added. The reaction was stirred at 0 ° C. for 2 h, and then the reaction was stopped with a saturated aqueous ammonium chloride solution. The resulting mixture was diluted with ethyl acetate and filtered through Chem Elut, and rinsed with additional ethyl acetate. The solvent was evaporated from the filtrate under reduced pressure, and the residue was purified by preparative HPLC to give 23 mg (7%) of 1- (2-benzyl-2-hydroxy-3-phenylbut-3-ene-1 -Yl) -1H-imidazole-5-carbonitrile.

MS(ESI)：330([M+H]+) MS (ESI): 330 ([M + H] + )

下表係以非限定的方式說明本發明化合物之實例。此等化合物係根據上述製備實例或以其類似法所製備。 The following table illustrates examples of the compounds of the present invention in a non-limiting manner. These compounds are prepared according to the above-mentioned preparation examples or in a similar manner.

LogP值：LogP value:

測量LogP值係根據EEC指令79/831 Annex V.A8藉由HPLC(高效液相層析)於逆相管柱上以下列方法來進行： The measurement of LogP value was performed by HPLC (High Performance Liquid Chromatography) on a reverse phase column according to EEC Directive 79/831 Annex V.A8:

[a]LogP值係藉由測量LC-UV，於酸性範圍，以0.1%甲酸溶於水和乙腈之溶液作為溶離劑所測(線性梯度從10%乙腈至95%乙腈)。 [a] LogP value is measured by measuring LC-UV in the acidic range with a solution of 0.1% formic acid in water and acetonitrile as the eluent (linear gradient from 10% acetonitrile to 95% acetonitrile).

[b]LogP值係藉由測量LC-UV，於中性範圍，以0.001莫耳濃度的乙酸銨於水和乙腈中之溶液作為溶離劑所測(線性梯度從10%乙腈至95%乙腈)。 [b] LogP value was measured by measuring LC-UV in the neutral range with a solution of ammonium acetate in water and acetonitrile at a concentration of 0.001 mol as the eluent (linear gradient from 10% acetonitrile to 95% acetonitrile) .

[c]LogP值係藉由測量LC-UV，於酸性範圍，以0.1%磷酸和乙腈作為溶離劑所測(線性梯度從10%乙腈至95%乙腈)。 [c] LogP values are measured by measuring LC-UV in the acidic range with 0.1% phosphoric acid and acetonitrile as eluents (linear gradient from 10% acetonitrile to 95% acetonitrile).

若在相同的方法內取得一個以上的的LogP值，則顯示所有的值並以「+」分開。 If more than one LogP value is obtained in the same method, all values are displayed and separated by "+".

以具有已知LogP值(使用滯留時間以連續烷酮間的線性內插測量LogP值)的直鏈烷2-酮(帶有3至16個碳原子)進行校正。使用200nm至400nm之UV-光譜及層析訊號的波峰值測定λ-最大-值。 Calibration was performed with a linear alkane 2-ketone (with 3 to 16 carbon atoms) with a known LogP value (measurement of LogP values using linear interpolation between consecutive alkane ketones). The λ-max-value was determined using the UV-spectrum of 200 nm to 400 nm and the peak value of the chromatographic signal.

NMR-波峰表NMR-peak table

所選實例之1H-NMR數據係以1H-NMR-波峰表的形式書寫。就各訊號峰係列出以ppm及以圓括號內的訊號強度表示的δ-值。成對的δ-值-訊號強度之間以分號作為分隔符號。 The 1 H-NMR data of the selected examples are written in the form of a 1 H-NMR-peak table. For each signal peak series, δ-values are expressed in ppm and the signal intensity in parentheses. The semi-colon is used as the separation symbol between the paired δ-value and signal strength.

實例的波峰表因此係具有下列形式：δ1(強度1)；δ2(強度2)；........；δi(強度i)；......；δn(強度n) The crest table of the example therefore has the following form: δ 1 (intensity 1 ); δ 2 (intensity 2 ); ........; δ i (intensity i ); ...; δ n ( Intensity n )

在一列印出的NMR光譜(以cm表示)之實例中尖銳的訊號強度係與訊號之高度有關且係顯示訊號強度的真正相關性。由寬訊號，可顯示與光譜中最強訊號相較之數個訊號的波峰或中間值及其相對強度。 In the example of a printed NMR spectrum (in cm), the sharp signal strength is related to the signal height and shows the true correlation of the signal strength. The wide signal can show the peak or middle value of several signals and their relative intensity compared with the strongest signal in the spectrum.

就校正1H光譜的化學位移，吾等係使用四甲基矽烷及/或所用溶劑之化學位移，特別是在以DMSO所測量的光譜之情況下。因此在NMR波峰表中，可能發生四甲基矽烷的波峰，但並非必定的。 To correct the chemical shift of the 1 H spectrum, we use the chemical shift of tetramethylsilane and / or the solvent used, especially in the case of the spectrum measured with DMSO. Therefore, in the NMR peak table, a peak of tetramethylsilane may occur, but it is not necessary.

1H-NMR波峰表係與正統的1H-NMR圖相類似且因此通常含有所有的波峰，其係以正統的NMR-解析圖列出。 The 1 H-NMR peak table is similar to the orthodox 1 H-NMR chart and therefore usually contains all the peaks, which are listed in the orthodox NMR-analysis chart.

另外，其可顯示如溶劑之正統的1H-NMR圖譜訊號、目標化合物之立體異構物，其亦為本發明之目標，及/或雜質之波峰值。 In addition, it can display signals such as orthodox 1H-NMR spectra of solvents, stereoisomers of target compounds, which are also targets of the present invention, and / or peaks of impurities.

顯示在溶劑及/或水之δ-範圍之化合物訊號，通常的溶劑之波峰值，例如DMSO-D6中之DMSO波峰值及水的波峰值係顯示在吾等之1H-NMR波峰值列表上且通常平均具有高強度。 Signals of compounds shown in the δ-range of solvents and / or water. The peaks of common solvents, such as the DMSO peak in DMSO-D 6 and the peak of water are shown on our 1H-NMR peak list. And usually has high strength on average.

目標化合物的立體異構物之波峰及/或雜質的波峰通常平均具有比目標化合物(例如具有純度>90%)之波峰較低的強度。 The peaks of the stereoisomers of the target compound and / or the peaks of the impurities generally have, on average, a lower intensity than the peaks of the target compound (eg, having a purity> 90%).

此等立體異構物及/或雜質可為特定製備程序之典型。因此，其波峰可經由「副產物指紋」幫助辨識吾等製備程序的再製。 These stereoisomers and / or impurities may be typical of a particular preparation procedure. Therefore, its peaks can help identify the reproduction of our preparation process through "by-product fingerprints".

熟習本項技術者，以已知的方法計算目標化合物之波峰(MestreC,ACD-模擬，但亦以經驗評估的期望值)，當需要時視需要使用另外的強度濾波器，可分離出目標化合物之波峰。此分離應類似於正統1H-NMR圖譜中的相關波峰擷取。 Those skilled in the art can calculate the peak of the target compound (MestreC, ACD-simulation, but also the expected value of empirical evaluation) by known methods, and use another intensity filter if necessary to isolate the target compound. crest. This separation should be similar to the correlation peak extraction in an orthodox 1 H-NMR spectrum.

波峰表之NMR-數據說明的進一步詳情，可參見出版刊物Research Disclosure Database Number 564025之“Citation of NMR Peaklist Data within Patent Applications”。 For further details of the NMR-data description of the wave table, please refer to the "Citation of NMR Peaklist Data within Patent Applications" published by Research Disclosure Database Number 564025.

生物實施例：Biological Example: 實施例A：甘藍鏈格孢菌(Alternaria brassicae)之預防試驗(蘿蔔或甘藍的葉斑)Example A: Alternaria brassicae prevention test (leaf spot of radish or cabbage)

溶劑：5體積%的二甲基亞碸 Solvent: 5 vol% dimethyl sulfene

10體積%的丙酮 10 vol% acetone

乳化劑：每毫克(mg)活性成份1μl的Tween® 80 Emulsifier: 1 μl of Tween ® 80 per milligram (mg) of active ingredient

將活性成份溶於二甲基亞碸/丙酮/Tween® 80之混合物中並均質化，及然後以水稀釋成所欲的濃度。 The active ingredient is dissolved in a mixture of dimethyl sulfene / acetone / Tween ® 80 and homogenized, and then diluted with water to the desired concentration.

將蘿蔔或甘藍的幼株藉由噴灑如上所製備的活性成份進行處理。對照組植株僅以丙酮/二甲基亞碸/Tween® 80的水溶液處理。 Young plants of radish or cabbage are treated by spraying the active ingredients prepared above. Control plants were treated only with an aqueous solution of acetone / dimethylmethylene / Tween ® 80.

24小時後，以甘藍鏈格孢菌孢子的水懸液噴灑葉片感染植株。將感染的蘿蔔或甘藍植株於20℃及100%相對濕度培養6天。 After 24 hours, the plants were infected by spraying the leaves with an aqueous suspension of Alternaria spores. The infected radish or cabbage was cultivated at 20 ° C and 100% relative humidity for 6 days.

於接種後6天評估此試驗。0%係指相當於對照組植株之效用，而100%之效用係指未觀察到罹病。 The test was evaluated 6 days after vaccination. 0% refers to the equivalent of the control plants, while 100% refers to the absence of disease.

在此試驗中，下列本發明化合物在500ppm之活性成份濃度時，顯現介於80%至89%的效用：I-12；I-13；I-14；I-18。 In this test, the following compounds of the present invention exhibited an effect between 80% and 89% at an active ingredient concentration of 500 ppm: I-12; I-13; I-14; I-18.

在此試驗中，下列本發明化合物在500ppm之活性成份濃度時，顯現介於90%至100%的效用：I-01；I-02；I-03；I-05；I-06；I-07；I-08；I-09；I-10；I-11；I-16；I-17；I-20。 In this test, the following compounds of the present invention exhibited an effect between 90% and 100% at an active ingredient concentration of 500 ppm: I-01; I-02; I-03; I-05; I-06; I- 07; I-08; I-09; I-10; I-11; I-16; I-17; I-20.

實施例B：活體內灰黴菌(Botrytis cinerea)(灰黴)之預防試驗Example B: Botrytis cinerea (Gray mold) prevention test in vivo

溶劑：5體積%的二甲基亞碸 Solvent: 5 vol% dimethyl sulfene

10體積%的丙酮 10 vol% acetone

乳化劑：每毫克(mg)活性成份1μl的Tween® 80 Emulsifier: 1 μl of Tween ® 80 per milligram (mg) of active ingredient

將活性成份溶於二甲基亞碸/丙酮/Tween® 80之混合物中並均質化，及然後以水稀釋成所欲的濃度。 The active ingredient is dissolved in a mixture of dimethyl sulfene / acetone / Tween ® 80 and homogenized, and then diluted with water to the desired concentration.

將醃漬用小黃瓜幼株藉由噴灑如上所製備的活性成份進行處理。對照組植株僅以丙酮/二甲基亞碸/Tween® 80的水溶液處理。 The pickled gherkin young plants are treated by spraying the active ingredients prepared as above. Control plants were treated only with an aqueous solution of acetone / dimethylmethylene / Tween ® 80.

24小時後，以灰黴菌孢子的水懸液噴灑葉片感染植株。將感染的小黃瓜植株於17℃及90%相對濕度培養4至5天。 After 24 hours, the plants were infected by spraying the leaves with an aqueous suspension of Botrytis spores. The infected gherkin plants were cultivated at 17 ° C and 90% relative humidity for 4 to 5 days.

於接種後4至5天評估此試驗。0%係指相當於對照組植株之效用，而100%之效用係指未觀察到罹病。 The test is evaluated 4 to 5 days after vaccination. 0% refers to the equivalent of the control plants, while 100% refers to the absence of disease.

在此試驗中，下列本發明化合物在500ppm之活性成份濃度時，顯現介於90%至100%的效用：I-01；I-02；I-03；I-05；I-06；I-08；I-09；I-10；I-11；I-16；I-20。 In this test, the following compounds of the present invention exhibited an effect between 90% and 100% at an active ingredient concentration of 500 ppm: I-01; I-02; I-03; I-05; I-06; I- 08; I-09; I-10; I-11; I-16; I-20.

實施例C：活體內隱匿柄銹菌(Puccinia recondita)(小麥褐銹病)之預防試驗Example C: Prevention test of Puccinia recondita (wheat brown rust) in vivo

溶劑：5體積%的二甲基亞碸 Solvent: 5 vol% dimethyl sulfene

10體積%的丙酮 10 vol% acetone

乳化劑：每毫克(mg)活性成份1μl的Tween® 80 Emulsifier: 1 μl of Tween ® 80 per milligram (mg) of active ingredient

將活性成份溶於二甲基亞碸/丙酮/Tween® 80之混合物中並均質化，及然後以水稀釋成所欲的濃度。 The active ingredient is dissolved in a mixture of dimethyl sulfene / acetone / Tween ® 80 and homogenized, and then diluted with water to the desired concentration.

將小麥幼株藉由噴灑如上所製備的活性成份進行處理。對照組植株僅以丙酮/二甲基亞碸/Tween® 80的水溶液處理。 Young wheat plants were treated by spraying the active ingredients prepared as above. Control plants were treated only with an aqueous solution of acetone / dimethylmethylene / Tween ® 80.

24小時後，以隱匿柄銹菌孢子的水懸液噴灑葉片感染植株。將感染的小麥植株於20℃和100%相對濕度培養24小時及然後於20℃和70-80%相對濕度培養10天。 After 24 hours, the plants were infected by spraying the leaves with an aqueous suspension of Puccinia spores. The infected wheat plants were cultivated at 20 ° C and 100% relative humidity for 24 hours and then at 20 ° C and 70-80% relative humidity for 10 days.

於接種後11天評估此試驗。0%係指相當於對照組植株之效用，而100%之效用係指未觀察到罹病。 This test was evaluated 11 days after vaccination. 0% refers to the equivalent of the control plants, while 100% refers to the absence of disease.

在此試驗中，下列本發明化合物在500ppm之活性成份濃度時，顯現介於80%至89%的效用：I-04。 In this test, at the active ingredient concentration of 500 ppm, the following compound of the present invention exhibited an effect ranging from 80% to 89%: I-04.

在此試驗中，下列本發明化合物在500ppm之活性成份濃度時，顯現介於90%至100%的效用：I-01；I-02；I-03；I-05；I-06；I-07；I-08；I-09；I-10；I-11；I-12；I-13；I-14；I-16；I-17；I-18；I-19；I-20。 In this test, the following compounds of the present invention exhibited an effect between 90% and 100% at an active ingredient concentration of 500 ppm: I-01; I-02; I-03; I-05; I-06; I- 07; I-08; I-09; I-10; I-11; I-12; I-13; I-14; I-16; I-17; I-18; I-19; I-20.

實施例D：活體內圓核腔菌(Pyrenophora teres)(大麥網紋病)之預防試驗Example D: Pyrenophora teres (barley reticulosis) prevention test in vivo

溶劑：5%體積比的二甲基亞碸 Solvent: 5% dimethyl sulfoxide by volume

10%體積比的丙酮 10% acetone by volume

乳化劑：每毫克(mg)活性成份1μl的Tween® 80/ Emulsifier: 1 μl of Tween ® 80 /

將活性成份溶於二甲基亞碸/丙酮/Tween® 80之混合物中並均質化，及然後以水稀釋成所欲的濃度。 The active ingredient is dissolved in a mixture of dimethyl sulfene / acetone / Tween ® 80 and homogenized, and then diluted with water to the desired concentration.

將大麥幼株藉由噴灑如上所製備的活性成份進行處理。對照組植株僅以丙酮/二甲基亞碸/Tween® 80的水溶液處理。 Young barley plants are treated by spraying the active ingredients prepared above. Control plants were treated only with an aqueous solution of acetone / dimethylmethylene / Tween ® 80.

24小時後，以圓核腔菌孢子的水懸液噴灑葉片感染植株。將感染的大麥植株於20℃和100%相對濕度培養48小時及然後於20℃和70-80%相對濕度培養12天。 After 24 hours, the plants were infected by spraying the leaves with an aqueous suspension of Coccidia spores. The infected barley plants were cultured at 20 ° C and 100% relative humidity for 48 hours and then at 20 ° C and 70-80% relative humidity for 12 days.

於接種後14天評估此試驗。0%係指相當於對照組植株之效用，而100%之效用係指未觀察到罹病。 The test was evaluated 14 days after vaccination. 0% refers to the equivalent of the control plants, while 100% refers to the absence of disease.

在此試驗中，下列本發明化合物在500ppm之活性成份濃度時，顯現介於80%至89%的效用：I-09；I-16；I-17。 In this test, the following compounds of the present invention exhibited an effect between 80% and 89% at an active ingredient concentration of 500 ppm: I-09; I-16; I-17.

在此試驗中，下列本發明化合物在500ppm之活性成份濃度時，顯現介於90%至100%的效用：I-01；I-02；I-03；I-06；I-08；I-10；I-11；I-13；I-14；I-20。 In this test, the following compounds of the present invention exhibited an effect between 90% and 100% at an active ingredient concentration of 500 ppm: I-01; I-02; I-03; I-06; I-08; I- 10; I-11; I-13; I-14; I-20.

實施例E：活體內小麥殼針孢菌(Septoria tritici)(小麥葉斑病)之預防試驗Example E: Prevention test of Septoria tritici (wheat leaf spot) in vivo

溶劑：5%體積比的二甲基亞碸 Solvent: 5% dimethyl sulfoxide by volume

10%體積比的丙酮 10% acetone by volume

乳化劑：每毫克(mg)活性成份1μl的Tween® 80 Emulsifier: 1 μl of Tween ® 80 per milligram (mg) of active ingredient

將活性成份溶於二甲基亞碸/丙酮/Tween® 80之混合物中並均質化，及然後以水稀釋成所欲的濃度。 The active ingredient is dissolved in a mixture of dimethyl sulfene / acetone / Tween ® 80 and homogenized, and then diluted with water to the desired concentration.

將小麥幼株藉由噴灑如上所製備的活性成份進行處理。對照組植株僅以丙酮/二甲基亞碸/Tween® 80的水溶液處理。 Young wheat plants were treated by spraying the active ingredients prepared as above. Control plants were treated only with an aqueous solution of acetone / dimethylmethylene / Tween ® 80.

24小時後，以小麥殼針孢菌孢子的水懸液噴灑葉片感染植株。將感染的小麥植株於18℃和100%相對濕度培養72小時及然後於20℃和90%相對濕度培養21天。 After 24 hours, the plants were infected by spraying the leaves with an aqueous suspension of H. spores spores. The infected wheat plants were cultured at 18 ° C and 100% relative humidity for 72 hours and then at 20 ° C and 90% relative humidity for 21 days.

於接種後19天評估此試驗。0%係指相當於對照組植株之效用，而100%之效用係指未觀察到罹病。 The test was evaluated 19 days after vaccination. 0% refers to the equivalent of the control plants, while 100% refers to the absence of disease.

在此試驗中，下列本發明化合物在500ppm之活性成份濃度時，顯現介於70%至79%的效用：I-04；I-16；I-18。 In this test, the following compounds of the present invention exhibited an effect between 70% and 79% at an active ingredient concentration of 500 ppm: I-04; I-16; I-18.

在此試驗中，下列本發明化合物在500ppm之活性成份濃度時，顯現介於80%至89%的效用：I-15；I-20。 In this test, the following compounds of the present invention exhibited an effect between 80% and 89% at an active ingredient concentration of 500 ppm: I-15; I-20.

在此試驗中，下列本發明化合物在500ppm之活性成份濃度時，顯現介於90%至100%的效用：I-01；I-02；I-03；I-05；I-06；I-07；I-08；I-09；I-10；I-11；I-13；I-14。 In this test, the following compounds of the present invention exhibited an effect between 90% and 100% at an active ingredient concentration of 500 ppm: I-01; I-02; I-03; I-05; I-06; I- 07; I-08; I-09; I-10; I-11; I-13; I-14.

實施例F：活體內灰花紋草單囊殼菌(Sphaerotheca fuliginea)(葫蘆科白粉病)之預防試驗Example F: Prevention test of Sphaerotheca fuliginea (Cucurbitaceae powdery mildew) in vivo

溶劑：5%體積比的二甲基亞碸 Solvent: 5% dimethyl sulfoxide by volume

10%體積比的丙酮 10% acetone by volume

乳化劑：每毫克(mg)活性成份1μl的Tween® 80 Emulsifier: 1 μl of Tween ® 80 per milligram (mg) of active ingredient

將活性成份溶於二甲基亞碸/丙酮/Tween® 80之混合物中並均質化，及然後以水稀釋成所欲的濃度。 The active ingredient is dissolved in a mixture of dimethyl sulfene / acetone / Tween ® 80 and homogenized, and then diluted with water to the desired concentration.

將醃漬用小黃瓜幼株藉由噴灑如上所製備的活性成份進行處理。對照組植株僅以丙酮/二甲基亞碸/Tween® 80的水溶液處理。 The pickled gherkin young plants are treated by spraying the active ingredients prepared as above. Control plants were treated only with an aqueous solution of acetone / dimethylmethylene / Tween ® 80.

24小時後，以灰花紋草單囊殼菌孢子的水懸液噴灑葉片感染植株。將感染的小黃瓜植株於20℃及70-80%相對濕度培養8天。 After 24 hours, the plants were infected by spraying the leaves with an aqueous suspension of S. gracilis spores. The infected gherkin plants were cultured at 20 ° C and 70-80% relative humidity for 8 days.

於接種後8天評估此試驗。0%係指相當於對照組植株之效用，而100%之效用係指未觀察到罹病。 The test was evaluated 8 days after vaccination. 0% refers to the equivalent of the control plants, while 100% refers to the absence of disease.

在此試驗中，下列本發明化合物在500ppm之活性成份濃度時，顯現介於90%至100%的效用：I-01；I-02；I-03；I-04；I-05；I-06；I-07；I-08；I-09；I-10；I-11；I-12；I-13；I-14；I-15；I-16；I-17；I-18；I-19；I-20。 In this test, the following compounds of the present invention exhibited an effect between 90% and 100% at an active ingredient concentration of 500 ppm: I-01; I-02; I-03; I-04; I-05; I- 06; I-07; I-08; I-09; I-10; I-11; I-12; I-13; I-14; I-15; I-16; I-17; I-18; I-19; I-20.

實施例G：活體內菜豆單胞銹菌(Uromyces appendiculatus)(菜豆銹並)之預防試驗Example G: Prevention test of Uromyces appendiculatus

溶劑：5%體積比的二甲基亞碸 Solvent: 5% dimethyl sulfoxide by volume

10%體積比的丙酮 10% acetone by volume

乳化劑：每毫克(mg)活性成份1μl的Tween® 80 Emulsifier: 1 μl of Tween ® 80 per milligram (mg) of active ingredient

將活性成份溶於二甲基亞碸/丙酮/Tween® 80之混合物中並均質化，及然後以水稀釋成所欲的濃度。 The active ingredient is dissolved in a mixture of dimethyl sulfene / acetone / Tween ® 80 and homogenized, and then diluted with water to the desired concentration.

將菜豆幼株藉由噴灑如上所製備的活性成份進行處理。對照組植株僅以丙酮/二甲基亞碸/Tween® 80的水溶液處理。 Young bean plants are treated by spraying the active ingredients prepared above. Control plants were treated only with an aqueous solution of acetone / dimethylmethylene / Tween ® 80.

24小時後，以菜豆單胞銹菌孢子的水懸液噴灑葉片感染植株。將感染的菜豆植株於20℃和100%相對濕度培養24小時及然後於20℃和70-80%相對濕度培養10天。 After 24 hours, the leaves were infected by spraying the leaves with water suspensions of P. leguminosus spores. Infected kidney bean plants were cultured at 20 ° C and 100% relative humidity for 24 hours and then at 20 ° C and 70-80% relative humidity for 10 days.

於接種後11天評估此試驗。0%係指相當於對照組植株之效用，而100%之效用係指未觀察到罹病。 This test was evaluated 11 days after vaccination. 0% refers to the equivalent of the control plants, while 100% refers to the absence of disease.

在此試驗中，下列本發明化合物在500ppm之活性成份濃度時，顯現介於80%至89%的效用：I-15。 In this test, at the active ingredient concentration of 500 ppm, the following compound of the present invention exhibited an effect ranging from 80% to 89%: I-15.

在此試驗中，下列本發明化合物在500ppm之活性成份濃度時，顯現介於90%至100%的效用：I-01；I-02；I-03；I-05；I-06；I-07；I-08；I-09；I-10；I-11；I-12；I-13；I-14；I-16；I-17；I-18；I-19；I-20。 In this test, the following compounds of the present invention exhibited an effect between 90% and 100% at an active ingredient concentration of 500 ppm: I-01; I-02; I-03; I-05; I-06; I- 07; I-08; I-09; I-10; I-11; I-12; I-13; I-14; I-16; I-17; I-18; I-19; I-20.

實施例H：活體內菜豆炭疽刺盤孢菌(Colletotrichum lindemuthianum)(菜豆葉斑病)之預防試驗Example H: Colletotrichum lindemuthianum (Phaseolus leaf spot) prevention test in vivo

溶劑：5%體積比的二甲基亞碸 Solvent: 5% dimethyl sulfoxide by volume

10%體積比的丙酮 10% acetone by volume

乳化劑：每毫克(mg)活性成份1μl的Tween® 80 Emulsifier: 1 μl of Tween ® 80 per milligram (mg) of active ingredient

將活性成份溶於二甲基亞碸/丙酮/Tween® 80之混合物中並均質化，及然後以水稀釋成所欲的濃度。 The active ingredient is dissolved in a mixture of dimethyl sulfene / acetone / Tween ® 80 and homogenized, and then diluted with water to the desired concentration.

將菜豆幼株藉由噴灑如上所製備的活性成份進行處理。對照組植株僅以丙酮/二甲基亞碸/Tween® 80的水溶液處理。 Young bean plants are treated by spraying the active ingredients prepared above. Control plants were treated only with an aqueous solution of acetone / dimethylmethylene / Tween ® 80.

24小時後，以菜豆炭疽刺盤孢菌孢子的水懸液噴灑葉片感染植株。將感染的菜豆植株於20℃和100%相對濕度培養24小時及然後於20℃和90%相對濕度培養6天。 After 24 hours, the leaves were infected by spraying the leaves with an aqueous suspension of A. anthracis spores. Infected kidney bean plants were cultivated at 20 ° C and 100% relative humidity for 24 hours and then at 20 ° C and 90% relative humidity for 6 days.

於接種後7天評估此試驗。0%係指相當於對照組植株之效用，而100%之效用係指未觀察到罹病。 The test was evaluated 7 days after vaccination. 0% refers to the equivalent of the control plants, while 100% refers to the absence of disease.

在此試驗中，下列本發明化合物在500ppm之活性成份濃度時，顯現介於70%至79%的效用：I-15。 In this test, the following compounds of the present invention exhibited an effect between 70% and 79% at an active ingredient concentration of 500 ppm: I-15.

在此試驗中，下列本發明化合物在500ppm之活性成份濃度時，顯現介於80%至89%的效用：I-05；I-08。 In this test, the following compounds of the present invention exhibited an effect between 80% and 89% at an active ingredient concentration of 500 ppm: I-05; I-08.

在此試驗中，下列本發明化合物在500ppm之活性成份濃度時，顯現介於90%至100%的效用：I-01；I-02；I-03；I-06；I-09；I-10；I-11；I-12；I-13；I-14；I-16；I-17；I-18；I-20。 In this test, the following compounds of the present invention exhibited an effect between 90% and 100% at an active ingredient concentration of 500 ppm: I-01; I-02; I-03; I-06; I-09; I- 10; I-11; I-12; I-13; I-14; I-16; I-17; I-18; I-20.

實施例I：活體內黑星菌(Venturia)(蘋果)之預防試驗Example I: Prevention test of Venturia (Apple) in vivo

溶劑：24.5重量份的丙酮 Solvent: 24.5 parts by weight of acetone

24.5重量份的二甲基乙醯胺 24.5 parts by weight of dimethylacetamide

乳化劑：1重量份的烷基芳基聚乙二醇醚 Emulsifier: 1 part by weight of alkylaryl polyethylene glycol ether

藉由將1重量份的活性化合物與所述量之溶劑和乳化劑混合，並將濃縮液以水稀釋成所欲的濃度，產生活性化合物之適合的製備物。 A suitable preparation of the active compound is produced by mixing 1 part by weight of the active compound with the amounts of the solvent and emulsifier and diluting the concentrate with water to a desired concentration.

將活性化合物之製備物以所述的施用率噴灑幼株，檢測預防效用。待噴灑層乾燥後，以蘋果黑星病致病原( Venturia inaequalis )的孢子水懸液接種植株，及然後在20℃和100%相對大氣溼度之培育箱中留置1天。 The preparations of the active compounds are sprayed on the young plants at the stated application rates to test the preventive effect. After the spray layer was dried, the plants were spore-watered with a spore suspension of Venturia inaequalis , and then left in an incubator at 20 ° C and 100% relative atmospheric humidity for 1 day.

然後將植株放置在大約21℃及大約90%相對大氣溼度之溫室中。 The plants were then placed in a greenhouse at approximately 21 ° C and approximately 90% relative atmospheric humidity.

於接種後10天評估此試驗。0%係指相當於對照組植株之效用，而100%之效用係指未觀察到罹病。 The test was evaluated 10 days after vaccination. 0% refers to the equivalent of the control plants, while 100% refers to the absence of disease.

在此試驗中，下列本發明化合物在100ppm之活性成份濃度時，顯現介於70%至79%的效用：I-03。 In this test, at the active ingredient concentration of 100 ppm, the following compound of the present invention exhibited an effect ranging from 70% to 79%: I-03.

在此試驗中，下列本發明化合物在100ppm之活性成份濃度時，顯現介於80%至89%的效用：I-13。 In this test, the following compounds of the present invention exhibited an effectiveness between 80% and 89% at an active ingredient concentration of 100 ppm: I-13.

在此試驗中，下列本發明化合物在100ppm之活性成份濃度時，顯現介於90%至100%的效用：I-01；I-02；I-05；I-06；I-08；I-10；I-11；I-14；I-16；I-17。 In this test, the following compounds of the present invention exhibited an effect between 90% and 100% at an active ingredient concentration of 100 ppm: I-01; I-02; I-05; I-06; I-08; I- 10; I-11; I-14; I-16; I-17.

實施例J：活體內預防性布氏白粉菌 (Blumeria)(大麥)試驗 Example J: In vivo prophylactic Blumeria (barley) test

溶劑：49重量份的N,N-二甲基乙醯胺 Solvent: 49 parts by weight of N, N-dimethylacetamide

乳化劑：1重量份的烷基芳基聚乙二醇醚 Emulsifier: 1 part by weight of alkylaryl polyethylene glycol ether

藉由將1重量份的活性化合物或活性化合物組合物與所述量之溶劑和乳化劑混合，並將濃縮液以水稀釋成所欲的濃度，產生活性化合物之適合的製備物。 A suitable preparation of the active compound is produced by mixing 1 part by weight of the active compound or active compound composition with the amounts of the solvent and emulsifier, and diluting the concentrate with water to a desired concentration.

將活性化合物或活性化合物組合物之製備物以所述的施用率噴灑幼株，檢測預防效用。 The active compound or the preparation of the active compound composition is sprayed on the young plants at the application rate to test the preventive effect.

待噴灑層乾燥後，將植株灑上大麥白粉菌( Blumeria graminis f.sp.hordei. )的孢子。 After the spray layer has dried, the plants are sprayed with spores of Blumeria graminis f.sp.hordei .

然後將植株放置在大約18℃之溫度及大約80%相對大氣溼度之溫室中，促進白粉膿皰發育。 The plants are then placed in a greenhouse at a temperature of about 18 ° C and a relative atmospheric humidity of about 80% to promote the development of powdery pustules.

於接種後7天評估此試驗。0%係指相當於對照組植株之效用，而100%之效用係指未觀察到罹病。 The test was evaluated 7 days after vaccination. 0% refers to the equivalent of the control plants, while 100% refers to the absence of disease.

在此試驗中，下列本發明化合物在500ppm之活性成份濃度時，顯現介於90%至100%的效用：I-01；I-02；I-03；I-05；I-06；I-08；I-14。 In this test, the following compounds of the present invention exhibited an effect between 90% and 100% at an active ingredient concentration of 500 ppm: I-01; I-02; I-03; I-05; I-06; 08; I-14.

Claims (14)

一種式(I)之化合物，
Figure TW201945344A_C0001
 其中R 1 係代表氫、C 1-C 8-烷基、C 2-C 8-烯基、C 2-C 8-炔基、C 3-C 8-環烷基、C 3-C 8-環烷基-C 1-C 4-烷基、C 1-C 8-烷氧基、C 1-C 8-烷硫基、C 6-C 14-芳基、C 6-C 14-芳基-C 1-C 4-烷基、C 6-C 14-芳基-C 2-C 4-烯基或C 6-C 14-芳基-C 2-C 4-炔基；其中R 1之脂肪族部分，不包括環烷基部分，可帶有1、2、3或至多最大可能數目之相同或不同的R a基團，其彼此獨立地係選自鹵素、CN、硝基、C 1-C 4-烷氧基和C 1-C 4-鹵基烷氧基；及其中R 1的環烷基及/或芳基部分可帶有1、2、3、4、5或至多最大可能數目之相同或不同的R b基團，其彼此獨立地係選自鹵素、CN、硝基、C 1-C 4-烷基、C 1-C 4-烷氧基、C 1-C 4-鹵烷基和C 1-C 4-鹵基烷氧基；R 2 係代表氫、鹵素、氰基或-OR 2a，其中R 2a 係代表氫、C 1-C 8-烷基、-Si(R 6a)(R 6b)(R 6c)、-P(O)(OH) 2、-CH 2-O-P(O)(OH) 2、-C(O)-C 1-C 8-烷基、-C(O)-C 3-C 7-環烷基、-C(O)NH-C 1-C 8-烷基、-C(O)N-二-C 1-C 8-烷基或-C(O)O-C 1-C 8-烷基，其中該-C(O)-C 1-C 8-烷基、-C(O)-C 3-C 7-環烷基、-C(O)NH-C 1-C 8-烷基、-C(O)N-二-C 1-C 8-烷基和-C(O)O-C 1-C 8-烷基為未經取代或經一或多個選自鹵素和C 1-C 8-烷氧基的基團取代，其中R 6a、R 6b、R 6c相互獨立地係代表苯基或C 1-C 8-烷基； R 3 係代表鹵素、羥基、氰基、異氰基、胺基、氫硫基(sulfanyl)、五氟-λ 6-氫硫基、羧醛、羥基羰基、C 2-C 8-烷基、C 1-C 8-鹵烷基、C 1-C 8-氰基烷基、C 1-C 8-烷基氧基、C 1-C 8-鹵烷基氧基、三(C 1-C 8-烷基)矽基、三(C 1-C 8-烷基)矽基-C 1-C 8-烷基、C 3-C 7-環烷基、C 3-C 7-鹵基環烷基、C 3-C 7-環烯基、C 3-C 7-鹵基環烯基、C 4-C 10-環烷基烷基、C 4-C 10-鹵基環烷基烷基、C 6-C 12-環烷基環烷基、C 1-C 8-烷基-C 3-C 7-環烷基、C 1-C 8-烷氧基-C 3-C 7-環烷基、三(C 1-C 8-烷基)矽基-C 3-C 7-環烷基、C 2-C 8-烯基、C 2-C 8-炔基、C 2-C 8-烯基氧基、C 2-C 8-鹵基烯基氧基、C 3-C 8-炔基氧基、C 3-C 8-鹵基炔基氧基、C 1-C 8-烷基胺基、C 1-C 8-鹵烷基胺基、C 1-C 8-氰基烷氧基、C 4-C 8-環烷基烷氧基、C 3-C 6-環烷氧基、C 1-C 8-烷基氫硫基、C 1-C 8-鹵烷基氫硫基、C 1-C 8-烷基羰基、C 1-C 8-鹵烷基羰基、芳基羰基、芳基-C 1-C 6-烷基羰基、C 3-C 8-環烷基羰基、C 3-C 8-鹵基環烷基羰基、胺甲醯基、C 1-C 8-烷基胺甲醯基、二-C 1-C 8-烷基胺甲醯基、N-C 1-C 8-烷基氧基胺甲醯基、C 1-C 8-烷氧基胺甲醯基、N-C 1-C 8-烷基-C 1-C 8-烷氧基胺甲醯基、胺基硫羰基、C 1-C 8-烷氧基羰基、C 1-C 8-鹵基烷氧基羰基、C 3-C 8-環烷氧基羰基、C 2-C 8-烷氧基烷基羰基、C 2-C 8-鹵基烷氧基烷基羰基、C 3-C 10-環烷氧基烷基羰基、C 1-C 8-烷基胺基羰基、二-C 1-C 8-烷基胺基羰基、C 3-C 8-環烷基胺基羰基、C 1-C 8-烷基羰基氧基、C 1-C 8-鹵烷基羰基氧基、C 3-C 8-環烷基羰基氧基、C 1-C 8-烷基羰基胺基、C 1-C 8-鹵烷基羰基胺基、C 1-C 8-烷基胺基羰基氧基、二-C 1-C 8-烷基胺基羰基氧基、C 1-C 8-烷基氧基羰基氧基、C 1-C 8-烷基亞磺醯基、C 1-C 8-鹵烷基亞磺醯基、C 1-C 8-烷基磺醯基、C 1-C 8-鹵烷基磺醯基、C 1-C 8-烷基磺醯基氧基、C 1-C 8-鹵烷基磺醯基氧基、C 1-C 8-烷基胺基胺磺醯基(C 1-C 8-alkylaminosulfamoyl)、二-C 1-C 8-烷基胺基胺磺醯基、(C 1-C 8-烷氧基亞胺基)-C 1-C 8-烷基、(C 3-C 7-環烷氧基亞胺基)-C 1-C 8-烷基、羥基亞胺基-C 1-C 8-烷基、(C 1-C 8-烷氧基亞胺基)-C 3-C 7-環烷基、羥基亞胺基-C 3-C 7-環烷基、(C 1-C 8-烷基亞胺基)-氧基、(C 1-C 8-烷基亞胺基)-氧基-C 1-C 8-烷基、(C 3-C 7-環烷基亞胺基)-氧基-C 1-C 8-烷基、(C 1-C 6-烷基亞胺基)-氧基-C 3-C 7-環烷基、(C 1-C 8-烯基氧基 亞胺基)-C 1-C 8-烷基、(C 1-C 8-炔基氧基亞胺基)-C 1-C 8-烷基、(苯甲氧基亞胺基)-C 1-C 8-烷基、C 1-C 8-烷氧基烷基、C 1-C 8-烷硫基烷基、C 1-C 8-烷氧基烷氧基烷基、C 1-C 8-鹵基烷氧基烷基、苯甲基、苯基、5-員雜芳基、6-員雜芳基、苯甲氧基、苯氧基、苯甲基氫硫基、苯甲基胺基、苯基氫硫基或苯基胺基，其中苯甲基、苯基、5-員雜芳基、6-員雜芳基、苯甲氧基或苯氧基為未經取代或經一或多個選自下列之基團取代：鹵素、羥基、氰基、異氰基、胺基、氫硫基、五氟-λ 6-氫硫基、羧醛、羥基羰基、C 1-C 8-烷基、C 1-C 8-鹵烷基、C 1-C 8-氰基烷基、C 1-C 8-烷基氧基、C 1-C 8-鹵烷基氧基、三(C 1-C 8-烷基)矽基、三(C 1-C 8-烷基)矽基-C 1-C 8-烷基、C 3-C 7-環烷基、C 3-C 7-鹵基環烷基、C 3-C 7-環烯基、C 3-C 7-鹵基環烯基、C 4-C 10-環烷基烷基、C 4-C 10-鹵基環烷基烷基、C 6-C 12-環烷基環烷基、C 1-C 8-烷基-C 3-C 7-環烷基、C 1-C 8-烷氧基-C 3-C 7-環烷基、三(C 1-C 8-烷基)矽基-C 3-C 7-環烷基、C 2-C 8-烯基、C 2-C 8-炔基、C 2-C 8-烯基氧基、C 2-C 8-鹵基烯基氧基、C 3-C 8-炔基氧基、C 3-C 8-鹵基炔基氧基、C 1-C 8-烷基胺基、C 1-C 8-鹵烷基胺基、C 1-C 8-氰基烷氧基、C 4-C 8-環烷基烷氧基、C 3-C 6-環烷氧基、C 1-C 8-烷基氫硫基、C 1-C 8-鹵烷基氫硫基、C 1-C 8-烷基羰基、C 1-C 8-鹵烷基羰基、芳基羰基、芳基-C 1-C 6-烷基羰基、C 3-C 8-環烷基羰基、C 3-C 8-鹵基環烷基羰基、C 1-C 8-烷基胺甲醯基、二-C 1-C 8-烷基胺甲醯基、N-C 1-C 8-烷基氧基胺甲醯基、C 1-C 8-烷氧基胺甲醯基、N-C 1-C 8-烷基-C 1-C 8-烷氧基胺甲醯基、胺基硫羰基、C 1-C 8-烷氧基羰基、C 1-C 8-鹵基烷氧基羰基、C 3-C 8-環烷氧基羰基、C 2-C 8-烷氧基烷基羰基、C 2-C 8-鹵基烷氧基烷基羰基、C 3-C 10-環烷氧基烷基羰基、C 1-C 8-烷基胺基羰基、二-C 1-C 8-烷基胺基羰基、C 3-C 8-環烷基胺基羰基、C 1-C 8-烷基羰基氧基、C 1-C 8-鹵烷基羰基氧基、C 3-C 8-環烷基羰基氧基、C 1-C 8-烷基羰基胺基、C 1-C 8-鹵烷基羰基胺基、C 1-C 8-烷基胺基羰基氧基、二-C 1-C 8-烷基胺基羰基氧基、C 1-C 8-烷基氧基羰基氧基、C 1-C 8-烷基亞磺醯基、C 1-C 8-鹵烷基亞磺醯基、C 1-C 8-烷基磺醯基、C 1-C 8-鹵烷基磺醯基、C 1-C 8-烷基磺醯基氧基、C 1-C 8-鹵烷基磺醯基氧基、C 1-C 8-烷基胺基胺磺醯基、二 -C 1-C 8-烷基胺基胺磺醯基、(C 1-C 8-烷氧基亞胺基)-C 1-C 8-烷基、(C 3-C 7-環烷氧基亞胺基)-C 1-C 8-烷基、羥基亞胺基-C 1-C 8-烷基、(C 1-C 8-烷氧基亞胺基)-C 3-C 7-環烷基、羥基亞胺基-C 3-C 7-環烷基、(C 1-C 8-烷基亞胺基)-氧基、(C 1-C 8-烷基亞胺基)-氧基-C 1-C 8-烷基、(C 3-C 7-環烷基亞胺基)-氧基-C 1-C 8-烷基、(C 1-C 6-烷基亞胺基)-氧基-C 3-C 7-環烷基、(C 1-C 8-烯基氧基亞胺基)-C 1-C 8-烷基、(C 1-C 8-炔基氧基亞胺基)-C 1-C 8-烷基、(苯甲氧基亞胺基)-C 1-C 8-烷基、C 1-C 8-烷氧基烷基、C 1-C 8-烷硫基烷基、C 1-C 8-烷氧基烷氧基烷基、C 1-C 8-鹵基烷氧基烷基、苯甲基、苯基、5-員雜芳基、6-員雜芳基、苯甲氧基、苯氧基、苯甲基氫硫基、苯甲基胺基、苯基氫硫基或苯基胺基；R 4 係代表氫、鹵素、C 1-C 8-烷基、C 1-C 8-鹵烷基、C 1-C 8-烷氧基、C 1-C 8-鹵基烷氧基、C 1-C 8-烷硫基或C 1-C 8-鹵基烷硫基；R 5 係代表氫、鹵素、C 1-C 8-烷基、C 1-C 8-鹵烷基、C 1-C 8-烷氧基、C 1-C 8-鹵基烷氧基、C 1-C 8-烷硫基或C 1-C 8-鹵基烷硫基；及Q 係代表式(Q-I)之6-員芳香環
Figure TW201945344A_C0002
 其中U 1 係代表CX 1或N；U 2 係代表CX 2或N；U 3 係代表CX 3或N；U 4 係代表CX 4或N；U 5 係代表CX 5或N；其中X 1、X 2、X 3、X 4、和X 5相互獨立地係代表氫、鹵素、硝基、氰基、氫硫基、五氟-λ 6-氫硫基、C 1-C 8-烷基、具有1至5個鹵素原子之C 1-C 8-鹵烷基、C 3-C 8-環烷基、具有1至5個鹵素原子之C 3-C 8-鹵基環烷基、 C 1-C 8-鹵烷基-C 3-C 7-環烷基、C 3-C 7-環烯基、C 2-C 8-烯基、C 2-C 8-炔基、C 6-C 12-二環烷基(bicycloalkyl)、C 3-C 8-環烷基-C 2-C 8-烯基、C 3-C 8-環烷基-C 2-C 8-炔基、C 1-C 8-烷氧基、具有1至5個鹵素原子之C 1-C 8-鹵基烷氧基、C 1-C 8-烷氧基羰基、C 1-C 8-鹵基烷氧基羰基、C 1-C 8-烷基次磺醯基(sulfenyl)、C 2-C 8-烯基氧基、C 3-C 8-炔基氧基、C 3-C 6-環烷氧基、C 1-C 8-烷基亞磺醯基、C 1-C 8-烷基磺醯基、三(C 1-C 8-烷基)-矽基氧基、三(C 1-C 8-烷基)-矽基、三(C 1-C 8-烷基)-矽基-C 2-C 8-炔基、三(C 1-C 8-烷基)-矽基-C 2-C 8-炔基氧基、C 6-C 14-芳基、C 6-C 14-芳基氧基、C 6-C 14-芳基次磺醯基、5-或6-員雜芳基、5-或6-員雜芳基氧基，其中C 6-C 14-芳基、C 6-C 14-芳基氧基、C 6-C 14-芳基次磺醯基、5-或6-員雜芳基、5-或6-員雜芳基氧基為未經取代或經一或多個選自下列之基團取代：鹵素、氰基氫硫基、五氟-λ 6-氫硫基、C 1-C 8-烷基、C 1-C 8-鹵烷基、C 1-C 8-氰基烷基、C 1-C 8-烷基氧基、C 1-C 8-鹵烷基氧基、三(C 1-C 8-烷基)矽基、三(C 1-C 8-烷基)矽基-C 1-C 8-烷基、C 3-C 7-環烷基、C 3-C 7-鹵基環烷基、C 3-C 7-環烯基、C 3-C 7-鹵基環烯基、C 4-C 10-環烷基烷基、C 4-C 10-鹵基環烷基烷基、C 6-C 12-環烷基環烷基、C 1-C 8-烷基-C 3-C 7-環烷基、C 1-C 8-烷氧基-C 3-C 7-環烷基、三(C 1-C 8-烷基)矽基-C 3-C 7-環烷基、C 2-C 8-烯基、C 2-C 8-炔基、C 2-C 8-烯基氧基、C 2-C 8-鹵基烯基氧基、C 3-C 8-炔基氧基、C 3-C 8-鹵基炔基氧基、C 1-C 8-氰基烷氧基、C 4-C 8-環烷基烷氧基、C 3-C 6-環烷氧基、C 1-C 8-烷基氫硫基、C 1-C 8-鹵烷基氫硫基、C 1-C 8-烷基亞磺醯基、C 1-C 8-鹵烷基亞磺醯基、C 1-C 8-烷基磺醯基、C 1-C 8-鹵烷基磺醯基、C 1-C 8-烷基磺醯基氧基、C 1-C 8-鹵烷基磺醯基氧基、C 1-C 8-烷氧基烷基、C 1-C 8-烷硫基烷基、C 1-C 8-烷氧基烷氧基烷基、C 1-C 8-鹵基烷氧基烷基、苯甲基、苯基、5-員雜芳基、6-員雜芳基、6-員雜芳基氧基、苯甲氧基、苯氧基、苯甲基氫硫基和苯基氫硫基，其中苯甲基、苯基、5-員雜芳基、6-員雜芳基、6-員雜芳基氧基、苯甲氧基、苯氧基、苯甲基氫硫基和苯基氫硫基為未經取代或經一或多個 選自鹵素、CN、硝基、C 1-C 8-烷基、C 1-C 4-鹵烷基、C 1-C 4-烷氧基、C 1-C 4-鹵基烷氧基和五氟-λ 6-氫硫基之基團取代；且其中U 1、U 2、U 3、U 4和U 5中最多二個係代表N；或U 1和U 2，或U 2和U 3，或U 3和U 4共同形成另外的飽和或不飽和的4至6-員經鹵素-或C 1-C 8-烷基取代或未經取代的環；及其鹽類和N-氧化物。 A compound of formula (I),
Figure TW201945344A_C0001
 Where R 1 represents hydrogen, C 1 -C 8 -alkyl, C 2 -C 8 -alkenyl, C 2 -C 8 -alkynyl, C 3 -C 8 -cycloalkyl, C 3 -C 8- Cycloalkyl-C 1 -C 4 -alkyl, C 1 -C 8 -alkoxy, C 1 -C 8 -alkylthio, C 6 -C 14 -aryl, C 6 -C 14 -aryl -C 1 -C 4 -alkyl, C 6 -C 14 -aryl-C 2 -C 4 -alkenyl or C 6 -C 14 -aryl-C 2 -C 4 -alkynyl; wherein R 1 aliphatic portion, excluding the cycloalkyl moiety, which may have up to three or identical or different groups R a maximum possible number of, independently from each other selected from halogen, CN, nitro, C 1 -C 4 -alkoxy and C 1 -C 4 -haloalkoxy; and the cycloalkyl and / or aryl portion of R 1 may carry 1, 2, 3, 4, 5 or up to the maximum possible The same or different numbers of R b groups are independently selected from halogen, CN, nitro, C 1 -C 4 -alkyl, C 1 -C 4 -alkoxy, C 1 -C 4- Haloalkyl and C 1 -C 4 -haloalkoxy; R 2 represents hydrogen, halogen, cyano or -OR 2a , where R 2a represents hydrogen, C 1 -C 8 -alkyl, -Si ( R 6a) (R 6b) ( R 6c), - P (O) (OH) 2, -CH 2 -OP (O) (OH) 2, -C (O) -C 1 -C 8 - alkyl -C (O) -C 3 -C 7 - cycloalkyl, -C (O) NH-C 1 -C 8 - alkyl, -C (O) N- two -C 1 -C 8 - alkyl or -C (O) OC 1 -C 8 -alkyl, wherein -C (O) -C 1 -C 8 -alkyl, -C (O) -C 3 -C 7 -cycloalkyl, -C ( O) NH-C 1 -C 8 -alkyl, -C (O) N-di-C 1 -C 8 -alkyl and -C (O) OC 1 -C 8 -alkyl are unsubstituted or Substitution of one or more groups selected from halogen and C 1 -C 8 -alkoxy, wherein R 6a , R 6b , R 6c independently of one another represent phenyl or C 1 -C 8 -alkyl; R 3 Represents halogen, hydroxy, cyano, isocyano, amine, sulfanyl, pentafluoro-λ 6 -hydrothio, carboxaldehyde, hydroxycarbonyl, C 2 -C 8 -alkyl, C 1 -C 8 -haloalkyl, C 1 -C 8 -cyanoalkyl, C 1 -C 8 -alkyloxy, C 1 -C 8 -haloalkyloxy, tri (C 1 -C 8- Alkyl) silyl, tri (C 1 -C 8 -alkyl) silyl-C 1 -C 8 -alkyl, C 3 -C 7 -cycloalkyl, C 3 -C 7 -halocycloalkyl , C 3 -C 7 -cycloalkenyl, C 3 -C 7 -halocycloalkenyl, C 4 -C 10 -cycloalkylalkyl, C 4 -C 10 -halocycloalkylalkyl, C 6 -C 12 -cycloalkylcycloalkyl, C 1 -C 8 -alkyl-C 3 -C 7 -cycloalkyl, C 1 -C 8 -alkoxy-C 3 -C 7 -cycloalkyl, tri (C 1 -C 8 -alkyl) silyl-C 3 -C 7 -cycloalkyl, C 2 -C 8 -alkenyl, C 2 -C 8 -alkynyl , C 2 -C 8 -alkenyloxy, C 2 -C 8 -haloalkenyloxy, C 3 -C 8 -alkynyloxy, C 3 -C 8 -haloalkynyloxy, C 1 -C 8 -alkylamino, C 1 -C 8 -haloalkylamino, C 1 -C 8 -cyanoalkoxy, C 4 -C 8 -cycloalkylalkoxy, C 3- C 6 -cycloalkoxy, C 1 -C 8 -alkylhydrothio, C 1 -C 8 -haloalkylhydrothio, C 1 -C 8 -alkylcarbonyl, C 1 -C 8 -halo Alkylcarbonyl, arylcarbonyl, aryl-C 1 -C 6 -alkylcarbonyl, C 3 -C 8 -cycloalkylcarbonyl, C 3 -C 8 -halocycloalkylcarbonyl, carbamate, C 1 -C 8 -alkylamine formamyl, di-C 1 -C 8 -alkylamine formamyl, NC 1 -C 8 -alkyloxyamine formamyl, C 1 -C 8 -alkane Oxyamine formamyl, NC 1 -C 8 -alkyl-C 1 -C 8 -alkoxyamine formamyl, aminothiocarbonyl, C 1 -C 8 -alkoxycarbonyl, C 1 -C 8 -haloalkoxycarbonyl, C 3 -C 8 -cycloalkoxycarbonyl, C 2 -C 8 -alkoxyalkylcarbonyl, C 2 -C 8 -haloalkoxyalkylcarbonyl, C 3 -C 10 -cycloalkoxyalkylcarbonyl , C 1 -C 8 -alkylaminocarbonyl, di-C 1 -C 8 -alkylaminocarbonyl, C 3 -C 8 -cycloalkylaminocarbonyl, C 1 -C 8 -alkylcarbonyl Oxy, C 1 -C 8 -haloalkylcarbonyloxy, C 3 -C 8 -cycloalkylcarbonyloxy, C 1 -C 8 -alkylcarbonylamino, C 1 -C 8 -haloalkyl Carbonylamino, C 1 -C 8 -alkylaminocarbonyloxy, di-C 1 -C 8 -alkylaminocarbonyloxy, C 1 -C 8 -alkyloxycarbonyloxy, C 1 -C 8 -alkylsulfinylsulfenyl, C 1 -C 8 -haloalkylsulfinylsulfenyl, C 1 -C 8 -alkylsulfinylsulfenyl, C 1 -C 8 -haloalkylsulfinyl, C 1 -C 8 -alkylsulfonyloxy, C 1 -C 8 -haloalkylsulfonyloxy, C 1 -C 8 -alkylaminoaminesulfonyl (C 1 -C 8- alkylaminosulfamoyl), di-C 1 -C 8 -alkylaminoaminesulfonyl, (C 1 -C 8 -alkoxyimino) -C 1 -C 8 -alkyl, (C 3 -C 7 -Cycloalkoxyimino) -C 1 -C 8 -alkyl, hydroxyimino-C 1 -C 8 -alkyl, (C 1 -C 8 -alkoxyimino) -C 3 -C 7 -cycloalkyl, hydroxyimino-C 3 -C 7 -cycloalkyl, (C 1 -C 8 -alkylimino) -oxy, (C 1 -C 8 -alkylimine Amine) -oxy-C 1 -C 8- Alkyl, (C 3 -C 7 -cycloalkylimino) -oxy-C 1 -C 8 -alkyl, (C 1 -C 6 -alkylimino) -oxy-C 3- C 7 -cycloalkyl, (C 1 -C 8 -alkenyloxyimino) -C 1 -C 8 -alkyl, (C 1 -C 8 -alkynyloxyimino) -C 1 -C 8 -alkyl, (benzyloxyimino) -C 1 -C 8 -alkyl, C 1 -C 8 -alkoxyalkyl, C 1 -C 8 -alkylthioalkyl, C 1 -C 8 -alkoxyalkoxyalkyl, C 1 -C 8 -haloalkoxyalkyl, benzyl, phenyl, 5-membered heteroaryl, 6-membered heteroaryl, Benzyloxy, phenoxy, benzylhydrothio, benzylamino, phenylhydrothio or phenylamino, of which benzyl, phenyl, 5-membered heteroaryl, 6- Heteroaryl, benzyloxy or phenoxy is unsubstituted or substituted with one or more groups selected from the group consisting of: halogen, hydroxyl, cyano, isocyano, amine, hydrogenthio, penta Fluoro-λ 6 -hydrothio, carboxaldehyde, hydroxycarbonyl, C 1 -C 8 -alkyl, C 1 -C 8 -haloalkyl, C 1 -C 8 -cyanoalkyl, C 1 -C 8 - alkyloxy, C 1 -C 8 - haloalkyl group, tri (C 1 -C 8 - alkyl) of silicon-based, tri (C 1 -C 8 - alkyl) -C 1 -C silicon based 8 -alkane Group, C 3 -C 7 -cycloalkyl, C 3 -C 7 -halocycloalkyl, C 3 -C 7 -cycloalkenyl, C 3 -C 7 -halocycloalkenyl, C 4 -C 10 -cycloalkylalkyl, C 4 -C 10 -halocycloalkylalkyl, C 6 -C 12 -cycloalkylcycloalkyl, C 1 -C 8 -alkyl-C 3 -C 7- Cycloalkyl, C 1 -C 8 -alkoxy-C 3 -C 7 -cycloalkyl, tris (C 1 -C 8 -alkyl) silyl-C 3 -C 7 -cycloalkyl, C 2 -C 8 -alkenyl, C 2 -C 8 -alkynyl, C 2 -C 8 -alkenyloxy, C 2 -C 8 -haloalkenyloxy, C 3 -C 8 -alkynyloxy , C 3 -C 8 -haloalkynyloxy, C 1 -C 8 -alkylamino, C 1 -C 8 -haloalkylamino, C 1 -C 8 -cyanoalkoxy, C 4 -C 8 -cycloalkylalkoxy, C 3 -C 6 -cycloalkoxy, C 1 -C 8 -alkylhydrothio, C 1 -C 8 -haloalkylhydrothio, C 1 -C 8 -alkylcarbonyl, C 1 -C 8 -haloalkylcarbonyl, arylcarbonyl, aryl-C 1 -C 6 -alkylcarbonyl, C 3 -C 8 -cycloalkylcarbonyl, C 3- C 8 -halocycloalkylcarbonyl, C 1 -C 8 -alkylaminomethyl, di-C 1 -C 8 -alkylaminomethyl, NC 1 -C 8 -alkyloxyamine Fluorenyl, C 1 -C 8 -alkoxyamine methylamyl, NC 1 -C 8 -alkyl-C 1 -C 8 -Alkoxyaminomethane, aminothiocarbonyl, C 1 -C 8 -alkoxycarbonyl, C 1 -C 8 -haloalkoxycarbonyl, C 3 -C 8 -cycloalkoxy Carbonyl, C 2 -C 8 -alkoxyalkylcarbonyl, C 2 -C 8 -haloalkoxyalkylcarbonyl, C 3 -C 10 -cycloalkoxyalkylcarbonyl, C 1 -C 8 -Alkylaminocarbonyl, di-C 1 -C 8 -alkylaminocarbonyl, C 3 -C 8 -cycloalkylaminocarbonyl, C 1 -C 8 -alkylcarbonyloxy, C 1 -C 8 -haloalkylcarbonyloxy, C 3 -C 8 -cycloalkylcarbonyloxy, C 1 -C 8 -alkylcarbonylamino, C 1 -C 8 -haloalkylcarbonylamino, C 1- C 8 -alkylaminocarbonyloxy, di-C 1 -C 8 -alkylaminocarbonyloxy, C 1 -C 8 -alkyloxycarbonyloxy, C 1 -C 8 -alkylene Sulfonyl, C 1 -C 8 -haloalkylsulfinyl sulfenyl, C 1 -C 8 -alkylsulfonyl sulfenyl, C 1 -C 8 -haloalkylsulfonyl, C 1 -C 8 -alkane Sulfofluorenyloxy, C 1 -C 8 -haloalkylsulfonyloxy, C 1 -C 8 -alkylaminoaminesulfonyl, di-C 1 -C 8 -alkylaminoamine Sulfonyl, (C 1 -C 8 -alkoxyimino) -C 1 -C 8 -alkyl, (C 3 -C 7 -cycloalkoxyimino) -C 1 -C 8- Alkyl, hydroxyimino-C 1 -C 8 -alkyl, (C 1 -C 8 -alkoxyimino) -C 3 -C 7 -cycloalkyl, hydroxyimino-C 3- C 7 -cycloalkyl, (C 1 -C 8 -alkylimino) -oxy, (C 1 -C 8 -alkylimino) -oxy-C 1 -C 8 -alkyl, (C 3 -C 7 -cycloalkylimino) -oxy-C 1 -C 8 -alkyl, (C 1 -C 6 -alkylimino) -oxy-C 3 -C 7- Cycloalkyl, (C 1 -C 8 -alkenyloxyimino) -C 1 -C 8 -alkyl, (C 1 -C 8 -alkynyloxyimino) -C 1 -C 8 -Alkyl, (benzyloxyimino) -C 1 -C 8 -alkyl, C 1 -C 8 -alkoxyalkyl, C 1 -C 8 -alkylthioalkyl, C 1- C 8 -alkoxyalkoxyalkyl, C 1 -C 8 -haloalkoxyalkyl, benzyl, phenyl, 5-membered heteroaryl, 6-membered heteroaryl, benzyloxy Group, phenoxy, benzylhydrothio, benzylamino, phenylhydrothio or phenylamino; R 4 represents hydrogen, halogen, C 1 -C 8 -alkyl, C 1- C 8 -haloalkyl, C 1 -C 8 -alkoxy, C 1 -C 8 -haloalkoxy, C 1 -C 8 -alkylthio, or C 1 -C 8 -haloalkylthio ; R 5 represents hydrogen, halogen, C 1 -C 8 -alkyl, C 1 -C 8 -halane C 1 -C 8 -alkoxy, C 1 -C 8 -haloalkoxy, C 1 -C 8 -alkylthio or C 1 -C 8 -haloalkylthio; and Q represents 6-membered aromatic ring of formula (QI)
Figure TW201945344A_C0002
 Where U 1 represents CX 1 or N; U 2 represents CX 2 or N; U 3 represents CX 3 or N; U 4 represents CX 4 or N; U 5 represents CX 5 or N; where X 1 , X 2 , X 3 , X 4 , and X 5 independently of one another represent hydrogen, halogen, nitro, cyano, hydrogenthio, pentafluoro-λ 6 -hydrothio, C 1 -C 8 -alkyl, having a C 1 to 5 halogen atoms 1 -C 8 - haloalkyl, C 3 -C 8 - cycloalkyl group having a C 1 to 5 halogen atoms 3 -C 8 - cycloalkyl halo -alkyl, C 1 -C 8 -haloalkyl-C 3 -C 7 -cycloalkyl, C 3 -C 7 -cycloalkenyl, C 2 -C 8 -alkenyl, C 2 -C 8 -alkynyl, C 6 -C 12 -bicycloalkyl, C 3 -C 8 -cycloalkyl-C 2 -C 8 -alkenyl, C 3 -C 8 -cycloalkyl-C 2 -C 8 -alkynyl, C 1 -C 8 -alkoxy, C 1 -C 8 -haloalkoxy having 1 to 5 halogen atoms, C 1 -C 8 -alkoxycarbonyl, C 1 -C 8 -haloalkoxy Carbonyl, C 1 -C 8 -alkylsulfenyl, C 2 -C 8 -alkenyloxy, C 3 -C 8 -alkynyloxy, C 3 -C 6 -cycloalkoxy , C 1 -C 8 -alkylsulfinylsulfenyl, C 1 -C 8 -alkylsulfinylsulfonyl, tris (C 1 -C 8 -alkyl) -silyloxy, tris (C 1 -C 8 -alkyl)- Silyl, tri (C 1 -C 8 -alkyl) -silyl-C 2 -C 8 -alkynyl, tris (C 1 -C 8 -alkyl) -silyl-C 2 -C 8 -alkynyl Oxy, C 6 -C 14 -aryl, C 6 -C 14 -aryloxy, C 6 -C 14 -arylsulfenylfluorenyl, 5- or 6-membered heteroaryl, 5- or 6 -Membered heteroaryloxy, wherein C 6 -C 14 -aryl, C 6 -C 14 -aryloxy, C 6 -C 14 -arylsulfenyl, 5- or 6-membered heteroaryl , 5- or 6-membered heteroaryloxy is unsubstituted or substituted with one or more groups selected from halogen, cyanohydrothio, pentafluoro-λ 6 -hydrothio, C 1- C 8 -alkyl, C 1 -C 8 -haloalkyl, C 1 -C 8 -cyanoalkyl, C 1 -C 8 -alkyloxy, C 1 -C 8 -haloalkyloxy Tris (C 1 -C 8 -alkyl) silyl, tris (C 1 -C 8 -alkyl) silyl-C 1 -C 8 -alkyl, C 3 -C 7 -cycloalkyl, C 3 -C 7 -halocycloalkyl, C 3 -C 7 -cycloalkenyl, C 3 -C 7 -halocycloalkenyl, C 4 -C 10 -cycloalkylalkyl, C 4 -C 10 -Halocycloalkylalkyl, C 6 -C 12 -cycloalkylcycloalkyl, C 1 -C 8 -alkyl-C 3 -C 7 -cycloalkyl, C 1 -C 8 -alkoxy -C 3 -C 7 - cycloalkyl, tri (C 1 -C 8 - alkyl) silicon based -C 3 -C 7 - cycloalkyl Group, C 2 -C 8 - alkenyl, C 2 -C 8 - alkynyl, C 2 -C 8 - alkenyl group, C 2 -C 8 - alkenyl group having a halogen group, C 3 -C 8 - Alkynyloxy, C 3 -C 8 -haloalkynyloxy, C 1 -C 8 -cyanoalkoxy, C 4 -C 8 -cycloalkylalkoxy, C 3 -C 6 -cyclo alkoxy, C 1 -C 8 - alkyl mercapto, C 1 -C 8 - haloalkyl group hydrogen, C 1 -C 8 - alkylsulfinyl acyl, C 1 -C 8 - haloalkyl Sulfenylsulfenyl, C 1 -C 8 -alkylsulfonyl, C 1 -C 8 -haloalkylsulfonyl, C 1 -C 8 -alkylsulfonyloxy, C 1 -C 8 - haloalkyl acyl group sulfo, C 1 -C 8 - alkoxyalkyl, C 1 -C 8 - alkylthio group, C 1 -C 8 - alkoxy, alkoxyalkyl, C 1 -C 8 -haloalkoxyalkyl, benzyl, phenyl, 5-membered heteroaryl, 6-membered heteroaryl, 6-membered heteroaryloxy, benzyloxy, phenoxy Benzyl, benzylhydrothio and phenylhydrothio, of which benzyl, phenyl, 5-membered heteroaryl, 6-membered heteroaryl, 6-membered heteroaryloxy, benzyloxy , Phenoxy, benzylhydrothio, and phenylhydrothio are unsubstituted or selected from one or more of halogen, CN, nitro, C 1 -C 8 -alkyl, C 1- C 4 -haloalkyl, C 1 -C 4 -alkoxy, C 1 -C 4 -haloalkoxy, and pentafluoro-λ 6 -hydrothio groups are substituted; and wherein U 1 , U 2 , U 3 , U 4 and U 5 represent at most two of N; or U 1 and U 2 , or U 2 and U 3 , or U 3 and U 4 together to form another saturated or unsaturated 4 to 6- members halogen - or C 1 -C 8 - alkyl substituted or unsubstituted ring; and salts and N- oxides. 根據請求項1之式(I)化合物，其中R 1係代表C 1-C 8-烷基、C 1-C 8-鹵烷基、C 3-C 8-環烷基、C 6-C 14-芳基或C 6-C 14-芳基-C 1-C 4-烷基，其中R 1的環烷基及/或芳基部分可帶有1或2個相同或不同的R b基團，其彼此獨立地係選自鹵素、CN、硝基、C 1-C 4-烷基、C 1-C 4-烷氧基、C 1-C 4-鹵烷基和C 1-C 4-鹵基烷氧基。 A compound of formula (I) according to claim 1, wherein R 1 represents C 1 -C 8 -alkyl, C 1 -C 8 -haloalkyl, C 3 -C 8 -cycloalkyl, C 6 -C 14 -Aryl or C 6 -C 14 -aryl-C 1 -C 4 -alkyl, wherein the cycloalkyl and / or aryl portion of R 1 may carry 1 or 2 identical or different R b groups , Which are independently selected from the group consisting of halogen, CN, nitro, C 1 -C 4 -alkyl, C 1 -C 4 -alkoxy, C 1 -C 4 -haloalkyl, and C 1 -C 4- Haloalkoxy. 根據請求項1和2中至少一項之式(I)化合物，其中R 2係代表-OR 2a，其中R 2a係代表氫或C 1-C 8-烷基。 A compound of formula (I) according to at least one of claims 1 and 2, wherein R 2 represents -OR 2a and wherein R 2a represents hydrogen or C 1 -C 8 -alkyl. 根據請求項1至3中至少一項之式(I)化合物，其中R 3係代表氟、氯、溴、碘、氰基、胺基硫羰基或C 1-C 4-鹵烷基。 A compound of formula (I) according to at least one of claims 1 to 3, wherein R 3 represents fluorine, chlorine, bromine, iodine, cyano, aminothiocarbonyl or C 1 -C 4 -haloalkyl. 根據請求項1至4中至少一項之式(I)化合物，其中R 4係代表氫或C 1-C 4-烷基而R 5係代表氫或C 1-C 4-烷基。 A compound of formula (I) according to at least one of claims 1 to 4, wherein R 4 represents hydrogen or C 1 -C 4 -alkyl and R 5 represents hydrogen or C 1 -C 4 -alkyl. 根據請求項1至5中至少一項之式(I)化合物，其中Q 係代表式(Q-I-1)至(Q-I-10)之6-員芳香環
Figure TW201945344A_C0003
Figure TW201945344A_C0004
 其中X 1、X 2、X 3、X 4和X 5係如請求項1中所定義。 A compound of formula (I) according to at least one of claims 1 to 5, wherein Q is a 6-membered aromatic ring of formulas (QI-1) to (QI-10)
Figure TW201945344A_C0003
Figure TW201945344A_C0004
 Where X 1 , X 2 , X 3 , X 4 and X 5 are as defined in claim 1. 根據請求項1至6中至少一項之式(I)化合物，其中Q 係代表式(Q-I-1)或(Q-I-2)之6-員芳香環
Figure TW201945344A_C0005
 其中X 1、X 2、X 3、X 4和X 5係如請求項1中所定義。 A compound of formula (I) according to at least one of claims 1 to 6, wherein Q represents a 6-membered aromatic ring of formula (QI-1) or (QI-2)
Figure TW201945344A_C0005
 Where X 1 , X 2 , X 3 , X 4 and X 5 are as defined in claim 1. 根據請求項1至7中至少一項之式(I)化合物，其中X 1、X 2、X 3、X 4和X 5相互獨立地係代表氫、鹵素、氰基、C 1-C 8-烷基、具有1至5個鹵素原子之C 1-C 8-鹵烷基、C 2-C 8-烯基、C 2-C 8-炔基、C 3-C 8-環烷基-C 2-C 8-烯基、C 3-C 8-環烷基-C 2-C 8-炔基、C 1-C 8-烷氧基、具有1至5個鹵素原子之C 1-C 8-鹵基烷氧基、C 6-C 14-芳基或C 6-C 14-芳基氧基，其中C 6-C 14-芳基和C 6-C 14-芳基氧基為未經取代或經一或多個選自鹵素、C 1-C 8-烷基、C 1-C 8-鹵烷基、C 1-C 8-烷基氧基和C 1-C 8-鹵烷基氧基之基團取代。 A compound of formula (I) according to at least one of claims 1 to 7, wherein X 1 , X 2 , X 3 , X 4 and X 5 independently of one another represent hydrogen, halogen, cyano, C 1 -C 8- Alkyl, C 1 -C 8 -haloalkyl having 1 to 5 halogen atoms, C 2 -C 8 -alkenyl, C 2 -C 8 -alkynyl, C 3 -C 8 -cycloalkyl-C 2 -C 8 - alkenyl, C 3 -C 8 - cycloalkyl, -C 2 -C 8 - alkynyl, C 1 -C 8 - alkoxy having a C 1 to 5 halogen atoms 1 -C 8 -Haloalkoxy, C 6 -C 14 -aryl or C 6 -C 14 -aryloxy, wherein C 6 -C 14 -aryl and C 6 -C 14 -aryloxy are unsubstituted Substituted or substituted by one or more selected from halogen, C 1 -C 8 -alkyl, C 1 -C 8 -haloalkyl, C 1 -C 8 -alkyloxy and C 1 -C 8 -haloalkyl Oxygen groups are substituted. 根據請求項1之式(I)化合物，其中R 1 係代表視需要經鹵素-或C 1-C 4-烷基-取代的C 3-C 7-環烷基，視需要經鹵素-或C 1-C 4-烷基-取代的苯基或視需要經鹵素-或C 1-C 4-烷基-取代的苯甲基；R 2 係代表-OH；R 3 係代表氰基或CF 3；R 4 係代表氫或甲基；R 5 係代表氫或甲基； 及Q 係代表式(Q-I-1)或(Q-I-2)之6-員芳香環
Figure TW201945344A_C0006
 其中X 1、X 2、X 3、X 4和X 5相互獨立地係代表氫、鹵素、氰基、C 1-C 8-烷基、具有1至5個鹵素原子之C 1-C 8-鹵烷基、C 2-C 8-烯基、C 2-C 8-炔基、C 3-C 8-環烷基-C 2-C 8-烯基、C 3-C 8-環烷基-C 2-C 8-炔基、C 1-C 8-烷氧基、C 1-C 8-具有1至5個鹵素原子之鹵基烷氧基、C 6-C 14-芳基或C 6-C 14-芳基氧基、其中C 6-C 14-芳基和C 6-C 14-芳基氧基為未經取代或經一或多個選自鹵素、C 1-C 8-烷基、C 1-C 8-鹵烷基、C 1-C 8-烷基氧基和C 1-C 8-鹵烷基氧基之基團取代；及其鹽類和N-氧化物。 A compound of formula (I) according to claim 1, wherein R 1 represents a C 3 -C 7 -cycloalkyl group optionally substituted with halogen- or C 1 -C 4 -alkyl-, and optionally halogen- or C 1 -C 4 -alkyl-substituted phenyl or optionally halogen- or C 1 -C 4 -alkyl-substituted benzyl; R 2 represents -OH; R 3 represents cyano or CF 3 R 4 represents hydrogen or methyl; R 5 represents hydrogen or methyl; and Q represents 6-membered aromatic ring of formula (QI-1) or (QI-2)
Figure TW201945344A_C0006
 Wherein X 1, X 2, X 3 , X 4 and X 5 independently of one another train represents hydrogen, halogen, cyano, C 1 -C 8 - alkyl groups having a C 1 to 5 halogen atoms 1 -C 8 - Haloalkyl, C 2 -C 8 -alkenyl, C 2 -C 8 -alkynyl, C 3 -C 8 -cycloalkyl-C 2 -C 8 -alkenyl, C 3 -C 8 -cycloalkyl -C 2 -C 8 -alkynyl, C 1 -C 8 -alkoxy, C 1 -C 8 -haloalkoxy having 1 to 5 halogen atoms, C 6 -C 14 -aryl or C 6- C 14 -aryloxy, wherein C 6 -C 14 -aryl and C 6 -C 14 -aryloxy are unsubstituted or selected from one or more halogens, C 1 -C 8- Group substitution of alkyl, C 1 -C 8 -haloalkyl, C 1 -C 8 -alkyloxy and C 1 -C 8 -haloalkyloxy; and salts and N-oxides thereof. 根據請求項9之式(I)化合物，其中R 1 係代表視需要經鹵素-取代的環丙基、視需要經鹵素-取代的苯基或視需要經鹵素-取代的苯甲基；及/或Q 係代表式(Q-I-1)之6-員芳香環
Figure TW201945344A_C0007
 其中X 1、X 2、X 3、X 4和X 5相互獨立地係代表氫、氟或氯。 A compound of formula (I) according to claim 9, wherein R 1 represents halogen-substituted cyclopropyl if necessary, halogen-substituted phenyl if necessary, or halogen-substituted benzyl if necessary; and / Or Q is 6-membered aromatic ring of representative formula (QI-1)
Figure TW201945344A_C0007
 Where X 1 , X 2 , X 3 , X 4 and X 5 independently represent hydrogen, fluorine or chlorine. 一種用於防治有害微生物，較佳地用於防治植物病原性有害真菌之組成物，其係包括0.01至99%重量比之至少一種根據請求項1、2、3、 4、5、6、7、8、9或10的式(I)化合物及1至99.99%重量比之至少一種載劑及/或界面活性劑。     A composition for controlling harmful microorganisms, preferably for controlling phytopathogenic harmful fungi, comprising 0.01 to 99% by weight of at least one according to claim 1, 2, 3, 4, 5, 6, 7 , 8, 9 or 10 compounds of formula (I) and at least one carrier and / or surfactant in a weight ratio of 1 to 99.99%.     一種用於作物保護和物料保護中防治有害微生物，較佳地植物病原性有害真菌之方法，其特徵在於將至少一種根據請求項1、2、3、4、5、6、7、8、9或10的式(I)化合物或根據請求項11的組成物施用於該有害微生物或其棲地。     A method for controlling harmful microorganisms, preferably phytopathogenic harmful fungi, in crop protection and material protection, characterized in that at least one of the methods according to claim 1, 2, 3, 4, 5, 6, 7, 8, 9 Or the compound of formula (I) of 10 or the composition according to claim 11 is applied to the harmful microorganism or its habitat.     一種根據至少一種請求項1、2、3、4、5、6、7、8、9或10之式(I)化合物或根據請求項11之組成物的用途，係用於作物保護和物料保護中防治有害微生物，較佳地植物病原性有害真菌。     A use of a compound of formula (I) according to at least one claim 1, 2, 3, 4, 5, 6, 7, 8, 9 or 10 or a composition according to claim 11 for crop protection and material protection Controlling harmful microorganisms, preferably phytopathogenic harmful fungi.     一種根據至少一種請求項1、2、3、4、5、6、7、8、9或10之式(I)化合物或根據請求項11之組成物的用途，係用於處理基因轉殖植物或用於處理種子。     A use of a compound of formula (I) according to at least one claim 1, 2, 3, 4, 5, 6, 7, 8, 9, or 10 or a composition according to claim 11, for treating a transgenic plant Or used to treat seeds.    
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