Bazedoxifene Acetate → Bazedoxifene

Participants

Reaction Conditions

Reaction Steps

Bazedoxifene acetate (2 g) and dimethylformamide (10 mL) are mixed and heated to 70-75° C. to produce a clear solution, followed by filtration. To the filtrate, toluene (400 mL), morpholine (1 mL), and water (100 mL) are added and the mixture is cooled to 0-10° C. and stirred overnight. The solid that forms is collected by filtration, washed with toluene (20 mL), and dried under vacuum below 80° C. for about 5 hours to afford crystalline bazedoxifene free base Form A (HPLC purity 99.2%, moisture content=0.32%).

Provenance & Evidence