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US 8,618,284 B2Granted
Methods of preparing polymorphic form A of bazedoxifene acetate
AssigneeWyeth
InventorsPaolo Andreella, Giuseppe Barreca, Francesco Tasinato, Massimo Verzini, Marco Demo, Fabio Bassan, Vincenzo Cannata, Giorgio Soriato, Roberto Brescello, Pietro Allegrini, Livius Cotarca
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Abstract
The present invention relates to methods of preparing polymorphic Form A of bazedoxifene acetate and polymorphic Form A prepared by such methods.
Claims17
A method of preparing polymorphic Form A of bazedoxifene acetate, the method comprising:
- (a) contacting hexamethylenimino benzyloxyindole with hydrogen in a solvent comprising ethanol, and in the presence of a catalyst at elevated temperature to provide a first reaction mixture comprising bazedoxifene free base, wherein the first reaction mixture is substantially free from hexamethylenimino benzyloxyindole, wherein step (a) is completed in less than about 10 hours;
- (b) treating said first reaction mixture with an antioxidant to provide a second reaction mixture;
- (c) filtering said second reaction mixture to provide a solution comprising bazedoxifene free base;
- and (d) treating said solution with acetic acid to crystallize polymorphic Form A of bazedoxifene acetate.
1 more element
Dependencies are inferred from the claim text.