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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Main Authors | , |
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Format | Patent |
Language | English |
Published |
06.03.1998
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Edition | 6 |
Subjects | |
Online Access | Get full text |
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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). |
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Bibliography: | Application Number: AU19970040144 |