Toluene → Bazedoxifene

Participants

Reaction Conditions

Reaction Steps

Bazedoxifene hydrochloride (50 g) and dimethylformamide (400 mL) are charged into a round bottomed flask, heated to about 70-75° C. and stirred for clear solution. The reaction mixture is cooled to 25-35° C. followed by addition of toluene (2500 mL), morpholine (50 mL) and water (1500 mL) and subsequently the mixture is stirred at room temperature for 12-24 hours. The solid formed is collected by filtration, washed with water (100 mL), toluene (100 mL) and dried under vacuum below 70° C. to afford crystalline bazedoxifene free base Form A of 99.65% HPLC purity.

Provenance & Evidence