期刊
JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS
卷 58, 期 11-12, 页码 433-441出版社
WILEY-BLACKWELL
DOI: 10.1002/jlcr.3346
关键词
omeprazole; esomeprazole; Prilosec; Nexium; tritium; hydrogen isotope exchange
Omeprazole (Prilosec (R)) 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 (R)), the active pure (S)-enantiomer of omeprazole.
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