Acetone → Bazedoxifene Acetate

Participants

Reaction Conditions

Reaction Steps

Bazedoxifene free base (700 mg) and acetone (8 mL) are mixed and stirred at 45-55° C. to make a clear solution. The solution is filtered followed by addition of seed crystals of bazedoxifene acetate (20 mg) and drop-wise addition of a mixture of acetic acid (0.1 mL) in acetone (1 mL) at room temperature. To the mixture, heptane (40 mL) is added over a period of 15-30 minutes and mixture is stirred for another 30 minutes. The solid so obtained is collected by filtration, washed with heptane (5 mL), and dried by suction. The obtained wet solid is then further dried under vacuum at below 70° C. for about 6-8 hours to afford 850 mg of crystalline bazedoxifene acetate Form D.

Provenance & Evidence