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- W1533562663 abstract "18 F‐labelled fluoroalkylamines are attractive reagents for the preparation of positron emission tomography tracers containing amine, amide, and N ‐heterocyclic moieties. Herein, we report that 2‐[ 18 F]fluoroethylamine can be obtained from 2‐[ 18 F]fluoroethyl azide by reduction with elemental copper under acidic conditions. Azide to amine reduction was achieved in near quantitative analytical yields within 30 min by heating a solution of 2‐[ 18 F]fluoroethyl azide in the presence of copper wire and aqueous trifluoroacetic acid. Subsequent reaction of 2‐[ 18 F]fluoroethylamine with benzoyl chloride in the presence of triethylamine provided N ‐[ 18 F]fluoroethyl benzamide in 63% decay‐corrected radiochemical yield from 2‐[ 18 F]fluoroethyl azide. The utility of the Cu(0)/H + azide reduction method was further exemplified by preparation of the potential GABA A tracer 9 H ‐β‐carboline N ‐2‐[ 18 F]fluoroethylamide, which was obtained in 46% decay‐corrected radiochemical yield by reaction of 2‐[ 18 F]fluoroethylamine with the corresponding 9 H ‐β‐carboline pentafluorophenyl ester. Copyright © 2012 John Wiley & Sons, Ltd." @default.
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- W1533562663 date "2012-07-01" @default.
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- W1533562663 title "Copper-mediated reduction of 2-[18F]fluoroethyl azide to 2-[18F]fluoroethylamine" @default.
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