发明名称 |
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 |
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. |
申请公布号 |
US2016280642(A1) |
申请公布日期 |
2016.09.29 |
申请号 |
US201615179086 |
申请日期 |
2016.06.10 |
申请人 |
Husain Mofazzal;G.S.C. Srikanth;Thorpunuri Swapna;Datta Debashish |
发明人 |
Husain Mofazzal;G.S.C. Srikanth;Thorpunuri Swapna;Datta Debashish |
分类号 |
C07D205/08;C12P17/10;C12P17/14;C07D263/26;C07C229/22 |
主分类号 |
C07D205/08 |
代理机构 |
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代理人 |
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主权项 |
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地址 |
Hyderabad IN |