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Base-catalyzed deuterium and tritium labeling of aryl methyl sulfones

✍ Scribed by John Scheigetz; Carl Berthelette; Chun Li; Robert J. Zamboni

Book ID: 102375091
Publisher: John Wiley and Sons
Year: 2004
Tongue: French
Weight: 118 KB
Volume: 47
Category: Article
ISSN: 0022-2135
DOI: 10.1002/jlcr.880

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✦ Synopsis

Abstract

A method is presented for conveniently tritiating the aryl methyl sulfones of compounds identified as potent and selective inhibitors of human Cox‐2 and as DP receptor antagonists. A base‐catalyzed exchange reaction was conducted with deuterated water and the total deuterium incorporation, ranging from 46 to 99%, was calculated using mass spectrometry. Results from these exchanges were used as guidelines for tritium labeling giving specific radioactivities in the range of 28–120 mCi/mmol (1.03–4.43 GBq/mmol). Copyright © 2004 John Wiley & Sons, Ltd.

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