H. Oinuma, K. Miyake, M. Yamanaka
Aug 1, 1990
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Journal
Journal of Labelled Compounds and Radiopharmaceuticals
Abstract
Syntheses of [phenyl-14C]4′-[[1-[2-(6-Methyl-2-pyridyl)ethyl]-4-piperidyl]carbonyl]methanesulfon-anilide dihydrochloride dihydrate (1) (14C-E-4031) and its pyridylpropyl analogue (2), that are selective class III antiarrhythmic agents, are described. A modified Michael reaction of (6), a key intermediate amine prepared from [U14C]aniline hydrochloride, with 6-methyl-2-vinylpyridine (7) and alkylation of (6) with 4-(3-chloropropyl) pyridine (8) respectively produced compounds, (1) and (2), in satisfactory yields.