Methanol → Bazedoxifene Acetate

Participants

Reaction Conditions

Reaction Steps

Crystalline bazedoxifene free base (5 g) is charged in methanol (100 mL) heated at reflux temperature to make a clear solution. The solution is filtered and cooled to 25-30° C. followed by addition of acetic acid (0.82 g). The reaction mixture is stirred for ˜1 hour followed by addition of seed crystals of Form D (250 mg). The reaction mixture is allowed to cool to 0-5° C. at which point water (200 mL) is slowly added over a period of 2 hours. The reaction mixture is maintained under stirring for another 1 hour at 0-5° C. The solid is collected by filtration and washed with water (10 mL), and dried under vacuum at about 90° C. to afford the title compound.

Provenance & Evidence