公开(公告)号：WO2013105118A8

公开(公告)日：2013-10-10

申请号：PCT/IN2013000021

申请日：2013-01-10

Applicant: COUNCIL SCIENT IND RES

Inventor： GADAKH SUNITA KHANDERAO ,  REKULA REDDY SANTHOSH ,  SUDALAI ARUMUGAM

IPC: C07D401/14 ,  C07D301/14 ,  C07D307/20 ,  C07D401/12 ,  C07D493/04

CPC classification number: C07D301/14 ,  C07C247/04 ,  C07D301/02 ,  C07D307/20 ,  C07D401/12 ,  C07D401/14 ,  C07D493/04

Abstract: 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).

Abstract translation: 本文公开了一种合成式5的syn叠氮化物环氧化物的新途径，其用作HIV蛋白酶抑制剂的不对称合成的常见中间体，例如安普那韦，福沙那韦，沙奎那韦和通过钴催化的水解获得的达伦那韦和帕利那韦的正式合成 外消旋的抗（2SR，3SR）-3-叠氮基-4-苯基-1,2-环氧丁烷（叠氮基 - 环氧化物）的动力学拆分。