Acetone → Bazedoxifene Acetate

Participants

Reaction Conditions

Reaction Steps

Bazedoxifene free base (2 g) and acetone (20 mL) are mixed and heated to 45-50° C. to produce a clear solution, which is filtered. The filtrate is cooled to 25-35° C. and seed crystals (20 mg) are added, followed by drop-wise addition of acetic acid (0.26 g). n-Heptane (50 mL) is added drop-wise over 30 minutes. The formed solid is collected by filtration, sequentially washed with n-heptane (10 mL), and then suction dried for 5 minutes. The wet solid is dried under vacuum at 70° C. for about 4-5 hours to afford 1.5 g of crystalline bazedoxifene acetate Form D.

Provenance & Evidence