Journal of Labelled Compounds and Radiopharmaceuticals 2015-01-01

Site selective syntheses of [(3)H]omeprazole using hydrogen isotope exchange chemistry.

Scott R Pollack, David J Schenk

Index: J. Labelled Comp. Radiopharm. 58 , 433-41, (2015)

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Abstract

Omeprazole (Prilosec®) is a selective and irreversible proton pump inhibitor used to treat various medical conditions related to the production of excess stomach acids. It functions by suppressing secretion of those acids. Radiolabeled compounds are commonly employed in the drug discovery and development process to support efforts including library screening, target identification, receptor binding, assay development and validation and safety assessment. Herein, we describe synthetic approaches to the controlled and selective labeling of omeprazole with tritium via hydrogen isotope exchange chemistry. The chemistry may also be used to prepare tritium labeled esomeprazole (Nexium®), the active pure (S)-enantiomer of omeprazole. Copyright © 2015 John Wiley & Sons, Ltd.