P. Conlon, W. Kiesman
Mar 30, 2007
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Journal
Journal of Labelled Compounds and Radiopharmaceuticals
Abstract
BG9928, a high affinity adenosine A1 antagonist, is currently in Phase II clinical trials for the treatment of congestive heart failure. A deuterium-labeled version of the molecule was synthesized and used as a standard for in vivo pharmacokinetic and in vitro metabolism studies. The labeled form of 3-[4-(2,6-dioxo-1,3-dipropyl-2,3,6,7-tetrahydro-1H-purin-8-yl)-bicyclo[2.2.2]oct-1-yl]-propionic acid (BG9928) was obtained in a convergent manner by joining two major building blocks: the specifically labeled heterocycle 5,6-diamino-1,3-dipropyl-1H-pyrimidine-2,4-dione (4) and the hemiester 4-(2-methoxycarbonyl-ethyl)-bicyclo[2.2.2]octane-1-carboxylic acid (10). Copyright © 2007 John Wiley & Sons, Ltd.