NOVEL PROCESS TO PREPARE INTERMEDIATES OF HIV-PROTEASE INHIBITORS THEREOF

摘要

The present invention relates to an industrially feasible and economically viable process for the preparation of (1S,2R)-3-[[4-aminophenyl)-sulfonyl](2-methylpropyl)amino]-2-hydroxy-1-(phenyl-methyl)propyl]amine of formula I and its salt thereof and optionally converting it to HIV-protease inhibitors like Darunavir, Amprenavir or its prodrug Fosamprenavir.;

主权项

1. A process for the preparation of diamino alcohol of formula I having purity greater than 99.8%,comprising the steps of:
a). reacting compound of formula II with reducing agent in suitable solvent; b). treating the reaction mixture with acid to form compound of formula III; c). optionally isolating compound of formula III; d). deprotecting compound of formula III; e). isolating compound of formula I; and f). optionally converting formula I into HIV-protease inhibitors like Darunavir, Amprenavir or its prodrug Fosamprenavir.