Acetic Acid → Bazedoxifene Acetate

Beteiligte Stoffe

Reaktionsbedingungen

Reaktionsschritte

Bazedoxifene free base from example 17 or from example 19 (10 g, 21.2 mmol) was suspended in acetone (80 ml) and heated to 50-55° C. After getting a clear solution, a mixture of acetic acid (1.4 g, 23.3 mmol) and acetone (10 ml) was added slowly. Then the reaction mixture was allowed to cool at 20-25° C., stirred for 2 hrs, filtered the product formed, washed with acetone (20 ml) and dried under vacuum to afford the title compound in high yield and high purity (12.7 g, 95%) M.R: 176-181° C. HPLC: 99.9%.

Herkunft & Nachweise