Patent ID: 8178665
Filing Date: 2012-05-15
Classification: C07D,C07F

Abstract:
1. A process for the preparation of ezetimibe of the Formula I comprising the following steps: a) converting 4-(4-fluorobenzoyl)-butyric acid of the Formula II into 4-[2-(4-fluorophenyl)-[1,3]dioxolane-2-yl]-butyric acid of the Formula IV through a non-isolated intermediate of Formula III, b) acylating a chiral compound of Formula V with the compound of Formula IV to obtain an acylated oxazolidinone derivative of the Formula VI, c) reacting the acylated oxazolidinone compound of Formula VI with a protected imine compound of Formula VII, and isolating the compound of Formula VIII, d) hydrolizing the ketal group of the compound of Formula IX to obtain a compound of Formula X, e) reducing enantioselectively the compound of general Formula X to obtain the compound of Formula XI, f) removing the silyl protecting group of the compound of the general Formula XI to obtain the end-product ezetimibe of the Formula I