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Synthesis of N-(2-piperidylmethyl)-2,5-BIS(2,2,2-trifluoroethoxy)benzamide-carbonyl-14C acetate (flecainide-14C acetate)

✍ Scribed by E. H. Banitt; G. J. Conard

Publisher
John Wiley and Sons
Year
1981
Tongue
French
Weight
281 KB
Volume
18
Category
Article
ISSN
0022-2135

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✦ Synopsis

Abstract

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.

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