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Synthesis of a tritium labelled antihistaminic drug [3H]-N,N-diethyl-2-[4-(phenylmethyl)phenoxy]-ethaneamine · HCl

✍ Scribed by J. T. Kovalainen; H. Morimoto; P. G. Williams; J. Vepsäläinen; A. Reijonen; J. Gynther

Publisher: John Wiley and Sons
Year: 1995
Tongue: French
Weight: 362 KB
Volume: 36
Category: Article
ISSN: 0022-2135
DOI: 10.1002/jlcr.2580361205

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✦ Synopsis

Abstract

A tritium labelled antihistamine, N,N‐diethyl‐2‐[4‐(phenylmethyl)phenoxy]‐ ethaneamine · HCl (DPPE, 4) was synthesized to investigate its binding characteristics to intracellular histamine receptors (H~IC~) and for further studies with specific ligands of H~IC~ to determine their potential effects on cell proliferation. A palladium catalyzed reduction of an activated carbonyl between the two phenyl groups of N,N‐diethyl‐2‐[4‐(benzoyl)phenoxy]‐ethaneamine · HCl (DBPE, 3) with 100% tritium gas was successful, where 55% øf the theoretical activity (specific activity 31.6 Ci/mmol) was obtained.

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