AN IMPROVED PROCESS FOR THE PREPARATION OF PAROXETINE AND ITS INTERMEDIATE

摘要

The present invention provides an improved process for the preparation of N-protected ((3S,4R)- 4-(4-fluorophenyl)piperidin-3-yl)methanol (compound (A)) and further its transformation to Paroxetine and its pharmaceutically acceptable salts. The process comprises reaction of compound (II) with amido-malonate compound (C) in the presence of a chiral catalyst and optionally a dehydrating agent to obtain compound (B); followed by reduction of (B) in the presence of a reducing agent to provide compound (A).