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

Article abstract of DOI:10.1002/jlcr.2580361205

A tritium labelled antihistamine, N,N-diethyl-2-[4-[phenylmethyl)phenoxyl- ethaneamine · HCl (DPPE, 4) was synthesized to investigate its binding characteristics 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% of the theoretical activity (specific activity 31.6 Ci/mmol) was obtained.