A novel process for preparation of darunavir and darunavir ethanolate of fine particle size

摘要

The present invention provides a novel process for preparation of darunavir that involves reduction of [(1S,2R)-3-[[(4-nitrophenyl)sulfonyl](2-methylpropyl)amino]-2-hydroxy -1-(phenylmethyl) propyl] carbamic acid (3R,3aS,6aR)-hexahydrofuro [2,3-b]furan-3-yl ester, of formula (5). The present invention also provides darunavir ethanolate of particle size wherein d is less than 130 µm, d is less than 30 µm, d is less than 10 µm and process for its preparation.