a novel process for the preparation of darunavir and particle size darunavir ethanolate.

摘要

a novel process for the preparation of darunavir and particle size darunavir ethanolate. The present invention provides a novel process for the preparation of darunavir which involves the reduction of [(1s, 2r) -3 - [[(4-nitrophenyl) sulfonyl] 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 d0.9 is less than 130 µm, d0.5 is less than 30 mm, d0.1 is less than 10 µm and process for its preparation.