Methanol → Bazedoxifene Acetate

Participants

Reaction Conditions

Reaction Steps

Crystalline bazedoxifene free base (15 g) is charged in a mixture of methanol (180 mL) and isopropyl alcohol (120 mL) and heated to reflux temperature to make a clear solution. The solution is filtered and cooled to about 25-30° C. over a period of 15 minutes followed by addition of acetic acid (1.91 g) and then seed crystals of Form D (0.75 g). Then the mixture is maintained at same temperature for about 20 minutes and then allowed to cool to 0° C. over a period of about 30 minutes. The solid is collected by filtration and dried under vacuum at about 80° C. for about 5 hours to afford the title compound having HPLC Purity of 99.80%. The obtained sample is analyzed by Scanning Electron Microscope and the image is depicted in FIG. 8.

Provenance & Evidence