The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.

The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.

Date of Patent:
Jun. 12, 2018

Filed:

Jun. 10, 2016
Applicant:

Mylan Laboratories Limited, Hyderabad, IN;

Inventors:

Mofazzal Husain, Hyderabad, IN;

Srikanth G. S. C., Hyderabad, IN;

Swapna Thorpunuri, Hyderabad, IN;

Debashish Datta, Hyderabad, IN;

Attorney:
Primary Examiner:
Assistant Examiner:
Int. Cl.
CPC ...
C07D 205/08 (2006.01); C12P 17/10 (2006.01); C12P 17/14 (2006.01); C07C 229/22 (2006.01); C07D 263/26 (2006.01); C12N 9/20 (2006.01);
U.S. Cl.
CPC ...
C07D 205/08 (2013.01); C07C 229/22 (2013.01); C07D 263/26 (2013.01); C12P 17/10 (2013.01); C12P 17/14 (2013.01); C12N 9/20 (2013.01); Y02P 20/55 (2015.11);
Abstract

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 compound (S)-5-(4-Fluoro-phenyl)-5-hydroxy-1 morpholin-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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