Hydrochloric Acid → Bendamustine Hydrochloride

Participants

Reaction Conditions

Reaction Steps

4-{5-[Bis-(2-chloroethyl)amino]-1-methyl-1H-benzimidazol-2-yl}-butyric acid isopropyl ester (4 g), is added to a mixture of water (13.6 mL) and concentrated hydrochloric acid (5.4 mL) in a round bottom flask. The mixture is heated to 40-45° C., maintained for 8 hours. Cooled the reaction mass to 25-30° C., stirred for 90 minutes, filtered, washed with water (12 mL), and dried under vacuum of 500-600 mm of Hg at 29° C. for 3 hours to give bendamustine hydrochloride. Yield: 2.7 g (75%).

Provenance & Evidence