http://rdf.ncbi.nlm.nih.gov/pubchem/patent/ES-2436662-T3

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publicationDate 2014-01-03-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber ES-2436662-T3
titleOfInvention Preparation procedures for polymorphic form A of bazedoxifene acetate
abstract A process for preparing polymorphic form A of bazedoxifene acetate, the procedure comprising: (a) contacting 1- (4- (2-azepan-1-yl) ethoxy) benzyl) -5- (benzyloxy) -2- (4- (benzyloxy) phenyl) -3-methyl-1H-indole 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, in which less 1% of 1- (4- (2-azepan-1-yl) ethoxy) benzyl) -5- (benzyloxy) -2- (4- (benzyloxy) phenyl) -3-methyl-1H-indole remains in the reaction mixture; (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 free base debazedoxifene; and (d) treating said solution with acetic acid, to crystallize Form A of bazedoxifene acetate in which the elevated temperature in step (a) is a temperature of 40 ° C to 60 ° C.
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