SYNTHESIS OF A TRITIUM-LABELED ANTIHISTAMINIC DRUG [H-3] (PHENYLAMETHYL)PHENOXY]-ETHANEAMINE-CENTER-DOT-HCL

A tritium labelled antihistamine, N,N-diethyl-2-[4-(phenyl- methyl)phe noxy]-ethaneamine . HCl (DPPE, 4) was synthesized to investigate its b inding intracellular histamine receptors (H-IC) and for further studie s with specific ligands of H-IC to determine their potential effects o n cell proliferation. A palladium catalyzed reduction of an activated carbonyl between the two phenyl groups of N,N-diethyl-2-[4-(benzoyl)ph enoxy]-ethaneamine . HCl (DBPE, 3) with 100% tritium gas was successfu l where 55% of the theoretical activity (specific activity 31.6 Ci/mmo l) was obtained.