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Synthesis of specifically deuterated adenosine A1 antagonist: BG9928

✍ Scribed by Patrick R. Conlon; William F. Kiesman

Publisher
John Wiley and Sons
Year
2007
Tongue
French
Weight
104 KB
Volume
50
Category
Article
ISSN
0022-2135

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✦ Synopsis

Abstract

BG9928, a high affinity adenosine A~1~ 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‐1__H__‐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‐1__H__‐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.

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