INDUSTRIAL PROCESS FOR THE PREPARATION OF BUPRENORPHINE AND ITS INTERMEDIATES

摘要

There is provided an efficient industrial process for the preparation of 21-cyclopropyl-7α-(2-hydroxy-3,3-dimethyl-2-butyl)-6,14-endo-ethano-6,7,8,14-tetrahydro-oripavine, i.e. buprenorphine of Formula-I in high yield and purity, with enhanced safety and eco-friendly norms. The invention further relates to an improved process for preparation of intermediates thereof in high yield and purity.;

主权项

1. A process for the preparation of a compound of Formula-I, comprising: contacting a compound of Formula-IX with an alkanethiol and a base in a first solvent to produce a compound of Formula-I: said contacting being carried out at a temperature between about 80° C. and about 150° C.