反应详情

温度

65 °C

Bazedoxifene hydrochloride (2 g) and dimethylsulfoxide (16 mL) are mixed and heated to 60-70° C. to produce a clear solution, followed by cooling to room temperature and filtration to make it particle free. To the filtrate, toluene (100 mL), aqueous sodium carbonate solution (10%, 5 mL) and water (50 mL) are added and the mixture is stirred at room temperature for solid formation. The solid so formed is collected by filtration, washed with toluene (5 mL), water (5 mL) and dried under vacuum below 80° C. to afford 1.7 g of crystalline bazedoxifene free base Form A.

1. customto produce a clear solution
2. temperatureby cooling to room temperature
3. filtrationfiltration
4. additionTo the filtrate, toluene (100 mL), aqueous sodium carbonate solution (10%, 5 mL) and water (50 mL) are added
5. customThe solid so formed
6. filtrationis collected by filtration
7. washwashed with toluene (5 mL), water (5 mL)
8. customdried under vacuum below 80° C.