Methanol → Bazedoxifene Acetate

Participants

Reaction Conditions

Reaction Steps

Crystalline bazedoxifene free base (35 g) is charged in a mixture of methanol (420 mL) and isopropyl alcohol (280 mL) and 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 (5.8 g) and then seed crystals of Form D (1.75 g). Further the mixture is stirred at the same temperature for about 20 minutes. The reaction mixture is then cooled to 0-5° C. over a period of about 30 minutes and stirred at the same temperature for 15-30 minutes. The solid is collected by filtration, washed with methanol (70 mL), and dried under vacuum at about 80° C. for 5-8 hours to afford the title compound.

Provenance & Evidence