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Synthesis of N‐(2‐piperidylmethyl)‐2,5‐BIS(2,2,2‐trifluoroethoxy)benzamide‐carbonyl‐ 14 C acetate (flecainide‐ 14 C acetate)
Author(s) -
Banitt E. H.,
Conard G. J.
Publication year - 1981
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.2580180513
Subject(s) - benzamide , chemistry , yield (engineering) , flecainide , ethyl acetate , carbon 14 , medicinal chemistry , nuclear chemistry , organic chemistry , medicine , materials science , metallurgy , atrial fibrillation , physics , cardiology , quantum mechanics
N‐(2‐Piperidylmethyl)‐2,5‐bis(2,2,2‐trifluoroethoxy)benzamide acetate (flecainide acetate; R‐818), a new antiarrhythmic agent, was labelled with carbon‐14 at the carboxamide position for metabolic studies. A three‐step synthetic route starting from 2,5‐dihydroxybenzoic acid‐carboxyl‐ 14 C provided chemically pure flecainide‐ 14 C acetate in 37.0% overall yield. Thin layer chromatographic analysis indicated that the carbon‐14 labelled product (12.28 mCi/mmol) was at least 99.5% radiochemically pure.