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US 9,309,210 B2Granted
Crystalline form of cabazitaxel and process for preparing the same
AssigneeAventis Pharma S.A.
InventorsEric Didier, Nicolas Tremaudeux, Lionel Zaske
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Abstract
The present invention relates to a novel crystalline ethyl acetate solvate form of cabazitaxel or 4α-acetoxy-2α-benzoyloxy-5β,20-epoxy-1β-hydroxy-7β,10β-dimethoxy-9-oxo-11-taxen-13α-yl(2R,3S)-3-tert-butoxycarbonylamino-2-hydroxy-3-phenylpropionate and process for preparing the same.
Claims1
A process for the preparation of a crystalline ethyl acetate solvate form of 4α-acetoxy-2α-benzoyloxy-5β,20-epoxy-1β-hydroxy-7β,10β-dimethoxy-9-oxo-11-taxen-13α-yl(2R,3S)-3-tert-butoxycarbonylamino-2-hydroxy-3-phenylpropionate comprising the following steps:
- having the 4α-acetoxy-2α-benzoyloxy-5β,20-epoxy-1β-hydroxy-7β,10β-dimethoxy-9-oxo-11-taxen-13α-yl(2R,3S)-3-tert-butoxycarbonylamino-2-hydroxy-3-phenylpropionate in solution in an organic solvent at room temperature;
- making a change of solvent to ethyl acetate at atmospheric or under reduced pressure;
- maintaining the so-formed solution in ethyl acetate on continued stirring, and
- recovering said crystalline ethyl acetate solvate form of 4α-acetoxy-2α-benzoyloxy-5β,20-epoxy-1β-hydroxy-7β,10β-dimethoxy-9-oxo-11-taxen-13α-yl(2R,3S)-3-tert-butoxycarbonylamino-2-hydroxy-3-phenylpropionate.
1 more element
Dependencies are inferred from the claim text.