反应详情

温度

65 °C

Bazedoxifene hydrochloride (1 g) and dimethylsulfoxide (10 mL) are mixed and heated to 60-70° C. to produce a clear solution, followed by filtration. To the filtrate, toluene (50 mL), morpholine (1 mL), and water (30 mL) are added and the mixture is stirred at room temperature for 12-24 hours. The solid so formed is collected by filtration, washed with toluene (5 mL), water (5 mL) and dried under vacuum below 80° C. for about 7 hours to afford 800 mg of crystalline bazedoxifene free base Form A.

1. customto produce a clear solution
2. filtrationfollowed by filtration
3. additionTo the filtrate, toluene (50 mL), morpholine (1 mL), and water (30 mL) are added
4. customThe solid so formed
5. filtrationis collected by filtration
6. washwashed with toluene (5 mL), water (5 mL)
7. customdried under vacuum below 80° C. for about 7 hours