Patent ID: 9126949
Filing Date: 2015-09-08
Classification: A61K,C07C,C07D

Abstract:
1. A process for the preparation of rilpivirine, which comprises: a. reacting the 4-(4-chloropyrimidin-2-ylamino)benzonitrile with (E)-3-(4-amino-3,5-dimethylphenyl)acrylonitrile hydrochloride in the presence of p-toluene sulfonic acid monohydrate and an ether solvent; b. heating the contents obtained in step (a) at above 90° C. to obtain a solution; c. cooling the solution obtained in step (b) at below 35° C.; d. basifying the solution with a base; e. extracting rilpivirine into organic solvent; f. removing the solvent from the solution obtained in step (e) to obtain a solid; g. slurrying the solid obtained in step (f) with a ketonic solvent, a nitrile solvent or mixture thereof; and h. isolating rilpivirine.