CSIR, INDIA-WO PATENT–synthesis of amprenavir and saquinavir

Originally posted on New Drug Approvals:

amprenavir

saquinavir

A process for synthesis of syn azido epoxide and its use as intermediate in the synthesis of amprenavir and saquinavir
Published as ———WO-2013105118
Council of Scientific & Industrial Research

http://worldwide.espacenet.com:80/publicationDetails/biblio?CC=WO&NR=2013105118A1&KC=A1&FT=D&DB=EPODOC&locale=en_EP&date=20130718&rss=true

Inventors

Gadakh, Sunita, Khanderao; Rekula, Reddy, Santhosh; Sudalai, Arumugam
Publication date 18-JUL-2013

HIV protease inhibitor

Disclosed herein is a novel route of synthesis of syn azide epoxide of formu 5, which is used as a common intermdeiate for asymmetric synthesis of HIV protease inhibitors such as Amprenavir, Fosamprenavir, Saquinavir and formal synthesis of Darunavir and Palinavir obtained by Cobalt- catalyzed hydrolyti kinetic resolution of racemic anti-(2SR, 3SR) – 3 -azido – 4 -phenyl – 1, 2- epoxybutane (azido-epoxide

IN2012DE82 10-JAN-2012 [priority]

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