Synthesis of tritium labeled 2,3,4,5‐tetrahydro‐1H‐3‐benzazepines

SKF 82526 (6-chloro-7,8-dihydroxy-1-(4-hydroxyphenyl)-2,3,4,5-tetrahydro-1H-3-benzazepine) has been synthesized in both racemic mono and enantiomerically pure ditritiated form; SKF 38393 (7,8-dihydroxy-1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepine) has also been labeled with tritium. In each case labeling was accomplished via tritiation of the appropriate ring halogenated precursor with tritium gas over Pd catalyst in triethylamine in DMF.