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Synthesis of a tritium labelled antihistaminic drug [ 3 H]‐N,N‐diethyl‐2‐[4‐(phenylmethyl)phenoxy]‐ethaneamine · HCl
Author(s) -
Kovalainen J. T.,
Morimoto H.,
Williams P. G.,
Vepsäläinen J.,
Reijonen A.,
Gynther J.
Publication year - 1995
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/jlcr.2580361205
Subject(s) - chemistry , tritium , antihistamine , histamine , tritium illumination , medicinal chemistry , palladium , specific activity , stereochemistry , catalysis , organic chemistry , enzyme , pharmacology , medicine , physics , nuclear physics
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.