发明授权
US09586893B2 Processes and intermediates for preparing a macrocyclic protease inhibitor of HCV
有权
制备HCV大环蛋白酶抑制剂的方法和中间体
- 专利标题： Processes and intermediates for preparing a macrocyclic protease inhibitor of HCV
- 专利标题（中）： 制备HCV大环蛋白酶抑制剂的方法和中间体
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申请号： US13634996申请日： 2011-03-16
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公开(公告)号： US09586893B2公开(公告)日： 2017-03-07
- 发明人: Dominic John Ormerod , Dominique Paul Michel Depre , Andras Horvath
- 申请人： Dominic John Ormerod , Dominique Paul Michel Depre , Andras Horvath
- 申请人地址： US NJ Titusville
- 专利权人： Janssen Pharmaceuticals
- 当前专利权人： Janssen Pharmaceuticals
- 当前专利权人地址： US NJ Titusville
- 代理商 Andrea Jo Kamage
- 优先权： EP10156681 20100316
- 国际申请： PCT/EP2011/053957 WO 20110316
- 国际公布： WO2011/113859 WO 20110922
- 主分类号： C07D493/08
- IPC分类号： C07D493/08 ; C07C255/57 ; C07C51/02 ; C07C51/41 ; C07C51/43 ; C07C67/03 ; C07C67/31 ; C07C69/757 ; C07C205/57 ; C07C215/30 ; C07C231/12 ; C07C235/40 ; C07C317/44 ; C07D251/28 ; C07D251/30 ; C07D309/30 ; C07D417/04 ; C07D417/14 ; C07D491/18 ; C07C201/12
摘要：
A process for preparing [(1R,2R)-4-oxo-1,2-cyclopentanedicarboxylic acid II, by the resolution of racemic 4-oxo-1,2-cyclopentanedicarboxylic acid (V), said process comprising: (a) reacting 4-oxo-1,2-cyclopentanedicarboxylic acid (V) with brucine or (1R,2S)-(−)-ephedrine, thus preparing the bis-brucine or bis-(1R,2S)-(−)-ephedrine salt of (V), and (b) precipitating selectively the bis-brucine or bis-(1R,2S)-(−)-ephedrine salt of (1R,2R)-4-oxo-1,2-cyclopentanedicarboxylic acid II, while the bis-brucine or bis-(1R,2S)-(−)-ephedrine salt of [(1S,2S)-4-oxo-1,2-cyclopentanedicarboxylic acid stays in solution; (c) liberating the acid II by removal of brucine or (1R,2S)-(−)-ephedrine from the precipitated salt obtained in step (b).
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