C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 205/08 (2006.01) A61K 31/397 (2006.01) C07C 229/22 (2006.01) C07D 263/26 (2006.01) C12P 17/00 (2006.01) C12P 17/10 (2006.01)
Patent
CA 2757722
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- 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.
La présente invention porte sur un procédé enzymatique permettant la préparation de la (S)-5-(4-fluorophényl)-5-hydroxy-1-morpholin-4-yl-pentan-1-one par réduction de la 1-(4-fluorophényl)-5-morpholin-4-yl-pentan-1,5-dione à l'aide d'une enzyme appropriée ou par dédoublement de la (R,S)-5-(4-fluorophényl)-5-hydroxy-1-morpholin-4-yl-pentan-1-one à l'aide d'une enzyme. L'invention porte également sur un procédé de préparation d'ézétimibe comportant les étapes de a) protection du composé (S)-5-(4-fluorophényl)-5-hydroxy-1-morpholin-4-yl-pentan-1-one par un groupe hydroxy-protecteur, b) hydrolyse du composé obtenu, c) condensation avec un agent auxiliaire chiral, d) réaction avec un composé imine protégé, e) conversion en ester d'alkyle, f) cyclisation et g) déprotection pour obtenir l'ézétimibe.
Debashish Datta
Gorantla Sarat Chandra Srikanth
Husain Mofazzal
Thorpunuri Swapna
Matrix Laboratories Ltd.
Rogers Law Office
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