Enzymatic process for obtaining 17 alpha- monoesters of cortexolone and/or its 9,11- dehydroderivatives
AssigneeCosmo S.p.A.
InventorsMauro Ajani, Luigi Moro
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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.
Claims20
Crystalline form I of cortexolone-17α-propionate characterized by a DRX as shown in FIG. 1, a DSC as shown in FIG. 2, and an IR as shown in FIG. 3.
A process for preparing crystalline Form I of cortexolone-17α-propionate, the process comprising crystallizing cortexolone-17α-propionate from tert-butylmethylether.
A pharmaceutical composition comprising crystalline form I of cortexolone-17α-propionate in association with at least one physiologically acceptable excipient.
Crystalline form IV of cortexolone-17α-propionate characterized by a DRX as shown in FIG. 30.
A process for preparing crystalline Form IV of cortexolone-17α-propionate, the process comprising crystallizing cortexolone-17α-propionate from a propylene glycol/water or polyethylene glycol/water mixture.
A pharmaceutical composition comprising crystalline form IV of cortexolone-17α-propionate, water, and at least one physiologically acceptable excipient.
Dependencies are inferred from the claim text.