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IT1399764B1 - Procedimento per la sintesi di 4h-imidazo [1,5-a][1,4]benzodiazepine, in particolare di midazolam. - Google Patents

Procedimento per la sintesi di 4h-imidazo [1,5-a][1,4]benzodiazepine, in particolare di midazolam.

Info

Publication number
IT1399764B1
IT1399764B1 ITMI2010A000777A ITMI20100777A IT1399764B1 IT 1399764 B1 IT1399764 B1 IT 1399764B1 IT MI2010A000777 A ITMI2010A000777 A IT MI2010A000777A IT MI20100777 A ITMI20100777 A IT MI20100777A IT 1399764 B1 IT1399764 B1 IT 1399764B1
Authority
IT
Italy
Prior art keywords
midazolam
benzodiazepine
imidazo
synthesis
procedure
Prior art date
Application number
ITMI2010A000777A
Other languages
English (en)
Inventor
Andrea Castellin
Paola Donnola
Michele Maggini
Original Assignee
F S I Fabbrica Italiana Sint
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by F S I Fabbrica Italiana Sint filed Critical F S I Fabbrica Italiana Sint
Priority to ITMI2010A000777A priority Critical patent/IT1399764B1/it
Priority to EP11162957A priority patent/EP2397470B1/en
Priority to IL212505A priority patent/IL212505A/en
Priority to US13/099,820 priority patent/US8557981B2/en
Priority to CN201110119221.7A priority patent/CN102241679B/zh
Publication of ITMI20100777A1 publication Critical patent/ITMI20100777A1/it
Application granted granted Critical
Publication of IT1399764B1 publication Critical patent/IT1399764B1/it

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
ITMI2010A000777A 2010-05-04 2010-05-04 Procedimento per la sintesi di 4h-imidazo [1,5-a][1,4]benzodiazepine, in particolare di midazolam. IT1399764B1 (it)

Priority Applications (5)

Application Number Priority Date Filing Date Title
ITMI2010A000777A IT1399764B1 (it) 2010-05-04 2010-05-04 Procedimento per la sintesi di 4h-imidazo [1,5-a][1,4]benzodiazepine, in particolare di midazolam.
EP11162957A EP2397470B1 (en) 2010-05-04 2011-04-19 Process for the synthesis of 4H-imidazo[1,5-a][1,4]benzodiazepines, in particular midazolam and salts thereof
IL212505A IL212505A (en) 2010-05-04 2011-04-26 Process for Synthesis of 4h - Imidazo [5,1– a] [4,1] Benzodiazepines, especially Midazolam and its salts
US13/099,820 US8557981B2 (en) 2010-05-04 2011-05-03 Process for the synthesis of 4H-imidazo [1,5-a] [1,4] benzodiazepines, in particular midazolam and salts thereof
CN201110119221.7A CN102241679B (zh) 2010-05-04 2011-05-04 合成4H-咪唑并[1,5-a][1,4]苯二氮*特别是咪达唑仑和其盐的方法

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
ITMI2010A000777A IT1399764B1 (it) 2010-05-04 2010-05-04 Procedimento per la sintesi di 4h-imidazo [1,5-a][1,4]benzodiazepine, in particolare di midazolam.

Publications (2)

Publication Number Publication Date
ITMI20100777A1 ITMI20100777A1 (it) 2011-11-05
IT1399764B1 true IT1399764B1 (it) 2013-05-03

Family

ID=43216970

Family Applications (1)

Application Number Title Priority Date Filing Date
ITMI2010A000777A IT1399764B1 (it) 2010-05-04 2010-05-04 Procedimento per la sintesi di 4h-imidazo [1,5-a][1,4]benzodiazepine, in particolare di midazolam.

Country Status (5)

Country Link
US (1) US8557981B2 (it)
EP (1) EP2397470B1 (it)
CN (1) CN102241679B (it)
IL (1) IL212505A (it)
IT (1) IT1399764B1 (it)

Families Citing this family (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN103319486B (zh) * 2012-03-22 2017-10-10 徐州市心血管病研究所 合成4H‑咪唑并[1,5‑a][1,4]苯二氮卓,特别是咪达唑仑的方法
JP7013446B2 (ja) 2016-08-16 2022-02-15 ユーダブリューエム・リサーチ・ファウンデーション，インコーポレーテッド Ｇａｂａ（ａ）受容体モジュレーター、及び、喘息における気道過敏及び炎症を抑制するための方法
CN108033964B (zh) * 2017-12-28 2021-02-09 杭州奥默医药股份有限公司 一种吡啶基咪唑并苯并二氮杂卓丙酸酯化合物及其合成和应用
CN111320632B (zh) * 2018-12-14 2021-06-01 江苏恩华药业股份有限公司 盐酸咪达唑仑的新晶型及其制备方法
CN111410658B (zh) * 2020-03-30 2021-03-26 江苏恩华药业股份有限公司 咪达唑仑或其药物组合物的杂质a和杂质b及其用途
CN113149992B (zh) * 2021-01-15 2023-05-16 福安药业集团重庆礼邦药物开发有限公司 一种盐酸咪达唑仑f晶型的制备方法及用途
CN113149914A (zh) * 2021-01-15 2021-07-23 福安药业集团重庆礼邦药物开发有限公司 一种咪达唑仑中间体脱氟杂质的制备方法
CN120623184A (zh) * 2021-05-20 2025-09-12 成都硕德药业有限公司 盐酸咪达唑仑新晶型及其制备方法
CN116041222B (zh) * 2021-09-02 2025-01-07 成都硕德药业有限公司 一种咪达唑仑的制备方法及其中间体
CN115232132B (zh) * 2022-07-25 2024-02-13 福安药业集团重庆礼邦药物开发有限公司 一种盐酸咪达唑仑g晶型及其制备方法
WO2024059669A2 (en) * 2022-09-13 2024-03-21 ODH IP Corp. Improved process for the preparation of imidazobenzodiazepines
WO2024077061A2 (en) * 2022-10-04 2024-04-11 Uwm Research Foundation, Inc. Gaba(a) receptor modulators and methods to control smooth muscle contraction and inflammation

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ZA755418B (en) * 1974-09-11 1977-06-29 Hoffmann La Roche Diazepine derivatives
US4280957A (en) * 1974-09-11 1981-07-28 Hoffmann-La Roche Inc. Imidazodiazepines and processes therefor
CA2184802C (en) * 1995-10-10 2007-07-31 Karl-Heinz Bender Process for manufacture of imidazo benzodiazepine derivatives
US20010014738A1 (en) * 1999-06-30 2001-08-16 Madhup K. Dhaon Process for the preparation of imidazodiazepine intermediates
US6512114B1 (en) * 1999-06-30 2003-01-28 Abbott Laboratories Process for the preparation of Midazolam
US6262260B1 (en) * 2000-03-23 2001-07-17 Abbott Laboratories Process for the preparation of midazolam
US7776852B2 (en) * 2007-09-11 2010-08-17 Chemagis Ltd. Process for producing highly pure midazolam and salts thereof

Also Published As

Publication number Publication date
CN102241679B (zh) 2014-08-13
IL212505A (en) 2013-11-28
ITMI20100777A1 (it) 2011-11-05
US8557981B2 (en) 2013-10-15
IL212505A0 (en) 2011-07-31
EP2397470A1 (en) 2011-12-21
EP2397470B1 (en) 2013-01-16
US20110275799A1 (en) 2011-11-10
CN102241679A (zh) 2011-11-16

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