Patent ID: 7687493
Filing Date: 2010-03-30
Classification: A61P,C07D

Abstract:
1. A process for the preparation of N-{1-[bis(4-chlorophenyl)methyl]azetidin-3-yl}-N-quinol-6-ylmethylsulfonamide dihydrochloride, which consists of the following steps: a) reacting 1-[bis(4-chlorophenyl)methyl]azetidin-3-ol hydrobromide with N-quinolin-6-ylmethanesulfonamide in the presence of diisopropyl azodicarboxylate (DIAD) and triphenylphosphine in toluene at a temperature in the range of from about 40 to about 60° C., to form N-{1-[bis(4-chlorophenyl)methyl]azetidin-3-yl}-N-quinol-6-ylmethylsulfonamide, b) removing toluene by azeotropic distillation with isopropanol; c) converting the N-{1-[bis(4-chlorophenyl)methyl]azetidin-3-yl}-N-quinol-6-ylmethylsulfonamide dihydrochloride by contacting it with 5-6 N hydrochloric acid; and d) crystallizing so formed N-{1-[bis(4-chlorophenyl)methyl]azetidin-3-yl}-N-quinol-6-ylmethylsulfonamide dihydrochloride.