发明授权
US08557981B2 Process for the synthesis of 4H-imidazo [1,5-a] [1,4] benzodiazepines, in particular midazolam and salts thereof
有权
合成4H-咪唑并[1,5-a] [1,4]苯并二氮杂卓的方法，特别是咪达唑仑及其盐
![Process for the synthesis of 4H-imidazo [1,5-a] [1,4] benzodiazepines, in particular midazolam and salts thereof](/docs/US/2013-10-15/US08557981B2/abs.jpg.600x600.jpg)
- 专利标题： Process for the synthesis of 4H-imidazo [1,5-a] [1,4] benzodiazepines, in particular midazolam and salts thereof
- 专利标题（中）： 合成4H-咪唑并[1,5-a] [1,4]苯并二氮杂卓的方法，特别是咪达唑仑及其盐
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申请号： US13099820申请日： 2011-05-03
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公开(公告)号： US08557981B2公开(公告)日： 2013-10-15
- 发明人: Andrea Castellin , Michele Maggini , Paola Donnola
- 申请人： Andrea Castellin , Michele Maggini , Paola Donnola
- 申请人地址： IT Alte di Montecchio Maggiore
- 专利权人： F.I.S. Fabbrica Italiana Sintetici S.p.A.
- 当前专利权人： F.I.S. Fabbrica Italiana Sintetici S.p.A.
- 当前专利权人地址： IT Alte di Montecchio Maggiore
- 代理机构： Dickstein Shapiro LLP
- 优先权： ITMI10A0777 20100504
- 主分类号： C07D487/12
- IPC分类号： C07D487/12
![Process for the synthesis of 4H-imidazo [1,5-a] [1,4] benzodiazepines, in particular midazolam and salts thereof](/abs-image/US/2013/10/15/US08557981B2/abs.jpg.150x150.jpg)
摘要：
The present invention refers to a process for the preparation of 4H-imidazo[1,5-a][1,4]benzodiazepines, in particular Midazolam, through an efficient and selective decarboxylation reaction of the derivative compound of the 5-aminomethyl-1-phenyl-1H-imidazole-4-carboxylic acid of formula (II) avoiding the formation of the 6H-imidazo[1,5-a][1,4]benzodiazepines by-products and the ensuing process for the isomerization of a 4H-imidazo[1,5-a][1,4]benzodiazepine product.
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