C. Palmer, J. Casida
Jul 1, 1991
Citations
0
Influential Citations
10
Citations
Journal
Journal of Labelled Compounds and Radiopharmaceuticals
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-[2,3-3H2]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-[2,3-3H2]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.