Acetone → Bazedoxifene Acetate

Participants

Reaction Conditions

Reaction Steps

Bazedoxifene free base (500 mg) and acetone (8 mL) are mixed and stirred at 50-60° C. to make a clear solution. The solution is filtered followed by addition of seed crystals of bazedoxifene acetate (10 mg) and drop-wise addition of acetic acid (0.12 mL). To the mixture, heptane (40 mL) is added over a period of 10 and mixture is stirred for another 10-15 minutes. The solid so obtained is collected by filtration, washed with heptane (10 mL), and dried by suction. The obtained wet solid is then further dried under vacuum at 65-70° C. for about 6-8 hours to afford 400 mg of crystalline bazedoxifene acetate Form D.

Provenance & Evidence