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Synthesis of carbon-14 labelled xenalipin - a potential hypolipidemic agent

✍ Scribed by John A. Hill; John F. Eaddy

Publisher
John Wiley and Sons
Year
1992
Tongue
French
Weight
288 KB
Volume
31
Category
Article
ISSN
0022-2135

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✦ Synopsis

Abstract

Xenalipin 1 (4′‐trifluoromethyl‐2‐biphenylcarboxylic acid) was synthesized in the [^14^C]‐labelled form with specific activity 21.0 mCi/mmol suitable for metabolism and distribution studies in animals. The synthetic sequence involved conversion of [^14^C]‐ benzoic acid to the 4,4‐dimethyl‐2‐oxazoline derivative, formation of an organozinc compound, palladium‐catalyzed coupling of the arylzinc‐oxazoline with 4‐trifluoromethyliodobenzene, and acid hydrolysis. The radiochemical purity was 99.4%.

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