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Novel selective catalytic reduction with tritium: Synthesis of the GABAA receptor radioligand 1-(4-ethynylphenyl)-4-[2,3-3H2]propyl-2,6,7-trioxabicyclo[2.2.2]octane

✍ Scribed by Christopher J. Palmer; John E. Casida

Publisher
John Wiley and Sons
Year
1991
Tongue
French
Weight
437 KB
Volume
29
Category
Article
ISSN
0022-2135

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✦ Synopsis

Abstract

Protection of the terminal alkyne function in 1‐(4‐ethynylphenyl)‐4‐(prop‐2‐enyl)‐2,6,7‐trioxabicyclo[2.2.2]octane with a trimethylsilyl group permits the selective catalytic reduction of the olefin moiety with tritium gas to give after deprotection 1‐(4‐ethynylphenyl)‐4‐[2,3‐^3^H~2~]propyl‐2,6,7‐trioxabicyclo‐[2.2.2]octane. The labeled product at high specific activity is an improved radioligand for the GABA‐gated chloride channel of insects and mammals and the intermediate 4‐[2,3‐^3^H~2~]propyl‐1‐[4‐[(trimethylsilyl)ethynyl]phenyl]‐2,6,7‐trioxabicyclo[2.2.2]octane is useful for studies on the metabolic activation of this selective proinsecticide.

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