METHOD OF OBTAINING 6BETA,7BETA,15BETA,16BETA-DIMETHYLENE-3-KETO-17ALPHA-PREGNENO-4-CARBOLACTON-21,17 DROSPIRENONE (DRSP) AS WELL AS 7ALPHA-(30HYDROXYPROPYL-1)-6BETA,7BETA,15BETA,16BETA-DIMETHYLENE5BETA-ANDROSTANOTRIOLE-3BETA,5,17BETA9ZK 92836) AND 6BETA,7BETA,15BETA,16BETA-DIMETHYLENE-5BETA-HYDROXY-17ALPHA-ANDROSTANOCARBOLACTON-21,17 AS INTERMEDIATE PRODUCTS OF THAT METHOD

摘要

Production of drospirenone (6beta ,7beta ;15beta ,16beta -dimethylene-3-oxo-17alpha -pregn-4-ene-21,17-carbolactone) of formula (I) comprises catalytically hydrogenating 17alpha -(3-hydroxy-1-propynyl)-6beta ,7beta ;15beta ,16beta -dimethylene-5beta -androstane-3beta ,5,17beta -triol of formula (II) to give 17alpha -(3-hydroxypropyl)-6beta ,7beta ;15beta ,16beta -dimethylene-5beta -androstane-3beta ,5,17beta -triol of formula (III), oxidising (III) in the presence of a ruthenium salt to give 6beta ,7beta ;15beta ,16beta -dimethylene-5beta -hydroxy-3-oxo-17alpha -pregnane-21,17-carbolactone of formula (IV), and dehydrating (IV): Also claimed are intermediates (III) and (IV).