PROCESS FOR THE PREPARATION OF DROSPIRENONE

摘要

It is described of a process for the preparation of drospirenone, the compound of formula 1 shown below, a synthetic steroid with progestogenic, antimineralocorticoid and antiandrogenic activity, useful for preparing pharmaceutical compositions having contraceptive action, starting from 17α-(3-hydroxypropyl)-6β,7β;15β,16β-dimethylene-5β-androstane-3β,5,17β-trioI.;

主权项

1. Process for the preparation of drospirenone comprising the following steps:
a) oxidation of the compound 17α-(3-hydroxypropyl)-6β,7β;15β,16β-dimethylene-5β-androstane-3β,5,17β-triol with an oxidizing agent in the presence of a catalytic amount of 2,2,6,6-tetramethylpiperidine-1-oxyl radical or a derivative thereof; b) removal of the solvent from the reaction mixture by distillation, obtaining a raw oily product containing 6β,7β;15β,16β-dimethylene-5β-hydroxy-3-oxo-17α-androstane-21,17-carbolactone; c) addition to said raw oily product of a mixture of water and an organic base and heating of the resulting mixture at a temperature comprised between 45 and 90° C., to form drospirenone.