Methanol → Bazedoxifene Acetate

Participants

Reaction Conditions

Reaction Steps

Crystalline bazedoxifene free base (20 g) is charged in a mixture of methanol (200 mL) and isopropyl alcohol (200 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 (3.31 g). The reaction mixture is stirred for 15-30 minutes and subsequently seed crystals of Form D (1 g) are added and further the mixture is stirred at the same temperature for about 30 minutes. The reaction mixture is then cooled to 0-5° C. over a period of 30 minutes and stirred at the same temperature for 15-30 minutes. The solid is collected by filtration and washed with pre-cooled mixture of methanol (10 mL) and isopropyl alcohol (10 mL), and dried under vacuum at about 90° C. for 5-8 hours to afford the title compound.

Provenance & Evidence