Synthesis of antiulcer drug esomeprazole.

Tran Huu Giap, To Hai Tung, Van Thi My Hue, Cao Thi Hue, Nguyen Thi Minh Hang, Chau Van Minh, Le Nguyen Thanh

Abstract


Esomeprazole (Nexium®), the (S)-isomer of Omeprazole, is the first proton-pump inhibitor developed as a single isomer for the treatment of acid-related diseases. It is used for the treatment of peptic ulcers, gastroesophagal reflux disease, and erosive esophagitis. Herein, we report our synthetic study of esomeprazole sodium salt from the starting    2-mercapto-5-methoxybenzimidazole and 2-(chloromethyl)-4-methoxy-3,5-dimethylpyridine hydrochloride reagents. The Esomeprazole sodium salt was obtained from enantioselectivesulfoxidation reaction in moderate yield with high enantioselectivity.


Keywords


Peptic Ulcer, Proton Pump Inhibitor, Omeprazole, Esomeprazole

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