Process for producing drospirenone (6È,7È;15È,16È-dimethylene-3-oxo-17alpha-pregn-4-en-21,17-carbolactone, LTuGTdrspLT/uGT), as well as 7alpha-(3-hydroxy-1-propyl)-6È,7È;15È,16È-dimethylene-5È-androstane-3È,5,17È-triol (LTuGTzk 92836LT/uGT) and

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, JORG-THORSTEN MOHR
Format Patent
LanguageEnglish
Published 06.03.1998
Edition6
Subjects
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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: AU19970040144