Patent ID: 8580981
Filing Date: 2013-11-12
Classification: A61P,C07D

Abstract:
1. A process for the preparation of darunavir of formula (A) or the ethanolate solvate thereof: which comprises: (i) reacting a compound of formula (1): wherein PG represents an amino protecting group, with N-benzyl-isobutylamine, namely a compound of formula (2): to obtain a compound of formula (3): (ii) treating the compound of formula (3) to remove the PG protecting group to obtain a compound of formula (4): (iii) coupling the compound of formula (4) with 1-([[(3R,3aS,6aR)hexahydrofuro[2,3-b]furan-3-yloxy]-carbonyl]oxy)-2,5-pyrrolidinedione of formula: to obtain compound of formula (5): (iv) removing the N-benzyl group from the compound of formula (5) to obtain a compound of formula (6): (v) introducing a p-nitrophenylsulfonyl group into the compound of formula (6) to obtain a compound of formula (7): (vi) reducing the nitro group of the compound of formula (7) to form darunavir (vii) and thereafter recrystallizing from ethanol if the ethanolate solvate is desired.