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


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.


Peptic Ulcer, Proton Pump Inhibitor, Omeprazole, Esomeprazole

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