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    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
    1.
    发明申请
    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
    （S）-5-（4-氟 - 苯基）-5-羟基-1-吗啉-4-基 - 戊-1-酮的制备方法，EZETIMIBE的中间体和进一步转化成EZETIMIBE

    公开(公告)号：US20120028316A1

    公开(公告)日：2012-02-02

    申请号：US13262722

    申请日：2010-03-30

    申请人： Mofazzal Husain ,  G.S.C Srikanth ,  Swapna Thorpunuri ,  Datta Debashish

    发明人： Mofazzal Husain ,  G.S.C Srikanth ,  Swapna Thorpunuri ,  Datta Debashish

    IPC分类号： C12P17/14 ,  C07D263/26 ,  C07C229/40 ,  C07D205/08

    CPC分类号： C07D205/08 ,  C07C229/22 ,  C07D263/26 ,  C12N9/20 ,  C12P17/10 ,  C12P17/14 ,  Y02P20/55

    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.

    摘要翻译： 本发明提供了通过还原1-（4-氟苯基）-5-（4-氟 - 苯基）-5-羟基-1-吗啉-4-基 - 戊-1-酮制备（S）-5- - 苯基）-5-吗啉-4-基 - 戊烷-1,5-二酮通过使用合适的酶或通过（R，S）-5-（4-氟 - 苯基）-5-羟基-1-吗啉 -4-基 - 戊-1-酮。 本发明还提供了制备依泽替米贝的方法，包括以下步骤：a）用（S）-5-（4-氟 - 苯基）-5-羟基-1-吗啉-4-基 - 戊-1-酮保护化合物 羟基保护基团b）水解所得化合物c）与手性助剂缩合d）与被保护的亚胺化合物反应e）转化为烷基酯f）环化并g）脱保护得到依泽替米贝。

    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
    3.
    发明申请
    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
    （S）-5-（4-氟 - 苯基）-5-羟基-1-吗啉-4-基 - 戊-1-酮的制备方法，EZETIMIBE的中间体和进一步转化成EZETIMIBE

    公开(公告)号：US20160280642A1

    公开(公告)日：2016-09-29

    申请号：US15179086

    申请日：2016-06-10

    申请人： Mofazzal Husain ,  Srikanth G.S.C. ,  Swapna Thorpunuri ,  Debashish Datta

    发明人： Mofazzal Husain ,  Srikanth G.S.C. ,  Swapna Thorpunuri ,  Debashish Datta

    IPC分类号： C07D205/08 ,  C12P17/10 ,  C12P17/14 ,  C07D263/26 ,  C07C229/22

    CPC分类号： C07D205/08 ,  C07C229/22 ,  C07D263/26 ,  C12N9/20 ,  C12P17/10 ,  C12P17/14 ,  Y02P20/55

    摘要： The present invention provides an enzymatic process for the preparation of (S)-5-(4-Fluoro-phenyl)-5-hydroxy-Imorpholin-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-1 morpholin-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 componnd (S)-5-(4-Fluoro-phenyl)-5-hydroxy-1 morpholin-4-yl-pentan-1-one with hydroxy protecting group b) hydrolyzing the obtained componnd c) condensing with a chiral auxiliary d) reacting with an protected imine componnd e) converting to alkyl ester f) cyclizing and g) deprotecting to obtain Ezetimibe.

    摘要翻译： 本发明提供了通过还原1-（4-氟苯基）-5-（4-氟 - 苯基）-5-羟基 - 吗啉-4-基 - 戊-1-酮制备（S） - 苯基）-5-吗啉-4-基 - 戊烷-1,5-二酮，通过使用合适的酶或通过（R，S）-5-（4-氟 - 苯基）-5-羟基-1 吗啉-4-基 - 戊-1-酮。 本发明还提供了制备依泽替米贝的方法，包括以下步骤：a）保护部分（S）-5-（4-氟 - 苯基）-5-羟基-1-吗啉-4-基 - 戊-1-酮 用羟基保护基b）水解得到的组分c）与手性助剂缩合d）与被保护的亚胺组分反应e）转化为烷基酯f）环化并g）脱保护得到依泽替米贝。