Acetone → Ticagrelor Fumarate

Participants

Reaction Conditions

Reaction Steps

Ticagrelor (0.5 g) and acetone (13 mL) were charged into a round bottom flask and the mixture was stirred at about 25-30° C. for about 15 minutes for clear solution. Then fumaric acid (0.12 g) was added to the above reaction mixture at 25-35° C. and mixture was stirred for 4-5 hours. To the clear solution, n-hexane (50 mL) was added and stirred for about 90 minutes for solid separation. The solid was filtered, washed with n-hexane (5 mL) and dried to afford the title compound in about 65% yield having chiral HPLC purity of about 99.8%.

Provenance & Evidence