ENZYMATIC PROCESS FOR OBTAINING 17 ALPHA- MONOESTERS OF CORTEXOLONE AND/OR ITS 9,11- DEHYDRODERIVATIVES
The present invention refers to a new enzymatic process for obtaining 17α-monoesters of cortexolone and/or its 9,11-dehydroderivatives starting from the corresponding 17α,21-diesters which comprises an enzymatic alcoholysis reaction. Furthermore, the present invention refers to new crystalline forms of cortexolone 17α-propionate and 9,11-dehydro-cortexolone 17α-butanoate.
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Page/Page column 5
(2011/05/03)
Lipase-catalyzed preparation of corticosteroid 17α-esters endowed with antiandrogenic activity
Several 17α-monoesters of cortexolone and its Δ9-derivative are endowed with antiandrogenic activity. Their synthesis can be accomplished by means of a lipase-catalyzed chemoselective alcoholysis of the corresponding 17α,21-diesters.
Ferraboschi, Patrizia,Mieri, Maria De,Ragonesi, Laura
p. 4610 - 4612
(2008/09/21)
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