Process for preparation of bicalutamide

摘要

The present invention discloses a process for the synthesis of N-[4-Cyano-3-(trifluoromethyl)phenyl]-3-[(4-fluorophenyl)sulphonyl]-2-hydroxy-2-methyl propanamide (Form I). The invention discloses a reagent for oxidation of N-[4-Cyano-3-(trifluoromethyl)phenyl]-3-[(4-fluorophenyl)thio]-2-hydroxy-2-methyl propanamide to N-[4-Cyano-3-(trifluoromethyl)phenyl]-3-[(4-fluorophenyl)sulphonyl]-2-hydroxy-2-methyl propanamide. More particularly, the invention discloses a method of purification of N-[4-Cyano-3-(trifluoromethyl)phenyl]-3-[(4-fluorophenyl)sulphonyl]-2-hydroxy-2-methyl propanamide in a mixture of methylethyl ketone and hexane giving form (I). This form (I) is useful as an active pharmaceutical and has antiandrogenic activity.