PROCESS FOR THE PREPARATION OF DROSPIRENON (6ÃY, 7ÃY; 15ÃY,16ÃY-DIMETHYLENE-3-OXO-17ALPHA-PREGN-4-ENE-21,17-CARBOLACTONE, DRSP)

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)...

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Bibliographic Details
Main Authors KLAUS NICKISCH, JÖRG-THORSTEN MOHR
Format Patent
LanguageEnglish
Portuguese
Published 26.08.2014
Subjects
CHEMISTRY
METALLURGY
ORGANIC CHEMISTRY
STEROIDS
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Summary: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).
Bibliography:Application Number: PT20090100011T