METHOD OF PREPARING ABIRATERONE ACETATE OF HIGH PURITY APPLICABLE ON INDUSTRIAL SCALE.

摘要

The solution relates to a method of preparing abiraterone acetate of formula I, which comprises: a) preparation of abiraterone of formula II by the Suzuki reaction of 3-pyridyldiethylborane and a halo steroid of formula VI or VII in the presence of a palladium catalytic system, a base, and a solvent; b) acetylation of abiraterone with formation of abiraterone acetate of formula I; c) isolation of abiraterone acetate by crystallization, wherein the palladium catalytic system consists of the catalyst palladium acetate - Pd(OAc)2 and the ligand triphenylphosphine - Ph3P.