发明授权
US09388440B2 Enzymatic process for the preparation of (S)-5-(4-fluoro-phenyl)-5-hydroxy-1morpholin-4-yl-pentan-1-one, an intermediate of Ezetimibe and further conversion to Ezetimibe
有权
制备（S）-5-（4-氟 - 苯基）-5-羟基-1-吗啉-4-基 - 戊-1-酮的酶法，依泽替米贝的中间体，并进一步转化为依泽替米贝
- 专利标题： Enzymatic process for the preparation of (S)-5-(4-fluoro-phenyl)-5-hydroxy-1morpholin-4-yl-pentan-1-one, an intermediate of Ezetimibe and further conversion to Ezetimibe
- 专利标题（中）： 制备（S）-5-（4-氟 - 苯基）-5-羟基-1-吗啉-4-基 - 戊-1-酮的酶法，依泽替米贝的中间体，并进一步转化为依泽替米贝
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申请号： US13262722申请日： 2010-03-30
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公开(公告)号： US09388440B2公开(公告)日： 2016-07-12
- 发明人: Mofazzal Husain , Sarat Chandra Srikanth Gorantla , Swapna Thorpunuri , Datta Debashish
- 申请人： Mofazzal Husain , Sarat Chandra Srikanth Gorantla , Swapna Thorpunuri , Datta Debashish
- 申请人地址： IN Hyderabad
- 专利权人： Mylan Laboratories Limited
- 当前专利权人： Mylan Laboratories Limited
- 当前专利权人地址： IN Hyderabad
- 优先权： IN760/CHE/2009 20090401; IN1994/CHE/2009 20090821; IN2502/CHE/2009 20091014
- 国际申请： PCT/IN2010/000203 WO 20100330
- 国际公布： WO2010/113175 WO 20101007
- 主分类号： C12P17/14
- IPC分类号： C12P17/14 ; C07D263/26 ; C12N9/20 ; C12P17/10
摘要：
The present invention provides an enzymatic process for the preparation of (S)-5-(4-Fluoro-phenyl)-5-hydroxy-1morpholin-4-yl-pentan-1-one by the reduction of 1-(4-Fluoro-phenyl)-5-morpholin-4-yl-pentane-1,5-dione by using a suitable enzyme or by the resolution of (R,S)-5-(4-Fluoro-phenyl)-5-hydroxy-1morpholin-4-yl-pentan-1-one by using an enzyme. The present invention also provides process for the preparation of Ezetimibe comprising the steps of a) protecting the compound (S)-5-(4-Fluoro-phenyl)-5-hydroxy-1morpholin-4-yl-pentan-1-one with hydroxy protecting group b) hydrolyzing the obtained compound c) condensing with a chiral auxiliary d) reacting with an protected imine compound e) converting to alkyl ester f) cyclizing and g) deprotecting to obtain Ezetimibe.
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