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KR840008801A - Method for preparing azole derivatives - Google Patents

Method for preparing azole derivatives Download PDF

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Publication number
KR840008801A
KR840008801A KR1019840002528A KR840002528A KR840008801A KR 840008801 A KR840008801 A KR 840008801A KR 1019840002528 A KR1019840002528 A KR 1019840002528A KR 840002528 A KR840002528 A KR 840002528A KR 840008801 A KR840008801 A KR 840008801A
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South Korea
Prior art keywords
acid addition
methoxy
compound
phenyl
dioxolane
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KR1019840002528A
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Korean (ko)
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KR870000276B1 (en
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헤르스 쟌 (외 1)
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폴 아드리안 쟌 쟈안센
쟈안센 파아마슈우티카 엔. 부이.
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Publication of KR840008801A publication Critical patent/KR840008801A/en
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Publication of KR870000276B1 publication Critical patent/KR870000276B1/en

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

내용 없음No content

Description

아졸 유도체의 제조방법Method for preparing azole derivatives

본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음Since this is an open matter, no full text was included.

Claims (3)

다음 일반식(Ⅳ)의 화합물 또는 다음 일반식(Ⅳ)의 금속염을 승온상태의 적합한 유기용매 중에서 다음 일반식(Ⅴ)의 화합물과 반응시키고; 또 화합물(Ⅳ)이 사전 염 형성을 행하지 않은 상태로 반응에 사용되는 경우에는 바람직하게는 과잉량의 아졸(Ⅳ)을 사용하거나 적합한 염기를 첨가해서 방출산을 고착시키며; 또 필요한 경우에는 적합한 산으로 반응시켜서 이같이 수득된 화합물(Ⅰ)의 약제학적 유용 산부가염을 제조하고;또 더 필요한 경우에는 표준공정에 따라 상기 생성물의 입체화학적 이성체를 제조함을 특징으로 해서 다음 일반식(Ⅰ)을 갖는 아졸 유도체, 이의 약제학적 혀용 산부가염 및 입체화학 적이성체로 구성되는 군으로부터 선정되는 화합물을 제조하는 방법.Reacting the compound of formula (IV) or a metal salt of formula (IV) with a compound of formula (V) in a suitable organic solvent at elevated temperature; When compound (IV) is used in the reaction without pre-salt formation, the release acid is preferably fixed by using an excess of azole (IV) or by adding a suitable base; If necessary, a pharmaceutically useful acid addition salt of Compound (I) thus obtained is prepared by reacting with a suitable acid; and if necessary, stereochemical isomers of the product are prepared according to a standard procedure. A method for preparing a compound selected from the group consisting of azole derivatives having formula (I), acid addition salts for pharmaceutical tongues and stereochemically isoforms thereof. 상기 일반식(Ⅰ), (Ⅳ) 및 (Ⅴ)에서, X는 CH 또는 N이고; Ar은 할로, 메틸 및 메톡시로 구성되는 군으로부터 독립적으로 선택된 1개 또는 2개의 레디칼로 임의 치환된 페닐기이며, R은 저급알킬 또는 저급알카노일 레디칼이고, 또 W는 반응성 에스테르 기능기이다.In the general formulas (I), (IV) and (V), X is CH or N; Ar is a phenyl group optionally substituted with one or two radicals independently selected from the group consisting of halo, methyl and methoxy, R is a lower alkyl or lower alkanoyl radical and W is a reactive ester functional group. 제1항에 있어서, 1H－이미다졸을 시스－1－아세틸－4－[4－〔[2－(브로모메틸)－2－(2,4－디클로로페닐)－1,3－디옥소란－4－일]메톡시]페닐]피페라진을 반응시키고 또 필요한 경우에는 이들 생성물의 치료제로 유용한 산부가염을 제조함을 특징으로 하여, (＋)－시스－아세틸－4-[4－[[2－(2,4－디클로로페닐)－2－(1H－이미다졸－1－일메틸)－1,3－디옥소란－4－일]메톡시]페닐]피페라진과 이의 약제학적으로 유용한 산부가염으로 구성으로 구성되는 군으로부터 선정된 화합물을 제조하는 방법.The 1H-imidazole according to claim 1, wherein 1H-imidazole is cis-1-acetyl-4- [4-[[2- (bromomethyl) -2- (2,4-dichlorophenyl) -1,3-dioxolane; (+)-Cis-acetyl-4- [4-[[], characterized by reacting the 4--4-yl] methoxy] phenyl] piperazine and, if necessary, preparing acid addition salts useful as therapeutic agents for these products. 2- (2,4-dichlorophenyl) -2- (1H-imidazol-1-ylmethyl) -1,3-dioxolane-4-yl] methoxy] phenyl] piperazine and its pharmaceutically useful A process for preparing a compound selected from the group consisting of acid addition salts. 제1항에 있어서, 1H－1,2,4－트리아졸 나트륨염을 시스－1－[4－[[2－(브로모메틸)－2－(2,4－디클로로페닐)－1,3－디옥소란－4－일]메톡시]페닐]－4－(1－메틸에틸)피페라진을 반응시키고, 또 필요한 경우에는 이들 생성물의 치료제로 유용한 산부가염을 제조함을 특징으로 하여 (＋)－시스－1－[4－[[2－(2,4－디클로로페닐)－2－(1H－1,2,4－트리아졸－1－일메틸)－1,3－디옥소란－4－일]메톡시]페닐]－4－(1－메틸에틸)피페라진과 이의 약제학적으로 유용한 산부가염으로 구성되는 군으로부터 선정된 화합물을 제조하는 방법.The 1H-1,2,4-triazole sodium salt is prepared in cis-1- [4-[[2- (bromomethyl) -2- (2,4-dichlorophenyl) -1,3]. -Dioxolane-4-yl] methoxy] phenyl] -4- (1-methylethyl) piperazine is reacted and, if necessary, an acid addition salt useful as a therapeutic agent for these products is produced. ) -Cis-1-[4-] [2- (2,4-dichlorophenyl) -2- (1H-1,2,4-triazol-1-ylmethyl) -1,3-dioxolane- 4-yl] methoxy] phenyl] -4- (1-methylethyl) piperazine and its pharmaceutically useful acid addition salts. ※ 참고사항 : 최초출원내용에 의하여 공개하는 것임.※ Note: The disclosure is based on the initial application.
KR1019840002528A 1983-05-18 1984-05-10 Process for preparing azole derivatives KR870000276B1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US49556583A 1983-05-18 1983-05-18
US495,565 1983-05-18
US495565 2000-02-01

Publications (2)

Publication Number Publication Date
KR840008801A true KR840008801A (en) 1984-12-19
KR870000276B1 KR870000276B1 (en) 1987-02-23

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ES (1) ES532501A0 (en)

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Publication number Publication date
ES8507542A1 (en) 1985-09-01
ES532501A0 (en) 1985-09-01
KR870000276B1 (en) 1987-02-23

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