Methanol → Bazedoxifene Acetate

Participants

Reaction Conditions

Reaction Steps

Crystalline bazedoxifene free base (10 g) is charged in a mixture of methanol (120 mL) and isopropyl alcohol (50 mL) and heated to reflux temperature to make a clear solution. The solution is filtered and cooled to about 27° C. over a period of 15 minutes followed by addition of acetic acid (1.65 g) and then seed crystals of Form D (0.5 g). Then the mixture is further allowed to cool to 0° C. over a period of about 2 hours. The reaction mixture is maintained at the same temperature for 1 hour and the solid is collected by filtration, washed with precooled methanol (20 mL), and dried under vacuum at about 70° C. for about 6 hours to afford the title compound having HPLC Purity of 99.84%.

Provenance & Evidence