PROCESS FOR PREPARING 17-SUBSTITUTED STEROIDS

摘要

The present invention relates to a process for the preparation of 17-substituted steroids and, more particularly, to an improved method of synthesizing abiraterone or derivatives thereof in high yield and purity by means of a key 3-formate intermediate.

主权项

1. A process for preparing abiraterone which comprises:
a) triflating a compound of formula (V):in the presence of a base to give a compound of formula (VI): b) contacting the crude compound of formula (VI) with a 3-pyridyl borane derivative under Suzuki cross-coupling conditions to give abiraterone 3β-formyloxy ester of formula (VII): c) hydrolysing the crude abiraterone 3β-formyloxy ester of formula (VII); and d) isolating a resulting abiraterone from an alcoholic solvent.