Enzymatic process for obtaining 17 alpha-monoesters of cortexolone and/or its 9,11-dehydroderivatives
AssigneeCosmo Dermatos Srl
InventorsAjani Mauro, Moro Luigi
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Abstract
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.
Claims29
A process for preparing cortexolone-17α-propionate in crystalline form III, said process comprising reacting a compound of formula II
- with a compound of formula III
- R′OH (III)
- in an organic solvent in the presence of a lipase from Candida to give cortexolone-17α-propionate, wherein R is CH3—CH2 and R′ is a linear aliphatic chain containing 1-10 carbon atoms and crystallizing said cortexolone-17α-propionate from a mixture of dichloromethane/n-hexane, or a mixture of acetone/n-hexane, or a mixture of ethanol/water, to give cortexolone-17α-propionate in crystalline form III.
Crystalline form III of cortexolone-17α-propionate having a DRX spectrum as represented in FIG. 7 or 10 or 13 and a DSC spectrum as represented in FIG. 8 or 11 or 14 and an IR spectrum as represented in FIG. 9 or 12 or 15.
Dependencies are inferred from the claim text.