Bazedoxifene Acetate → Bazedoxifene

関与物質

反応条件

反応手順

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%).

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