| Autor: |
Edward G. Robins, William Trigg, Alessandra Gaeta, Matthias Glaser, James Nairne, Erik Årstad |
| Rok vydání: |
2012 |
| Předmět: |
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| Zdroj: |
Journal of Labelled Compounds and Radiopharmaceuticals. 55:326-331 |
| ISSN: |
0362-4803 |
| DOI: |
10.1002/jlcr.2945 |
| Popis: |
18F-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-[18F]fluoroethylamine can be obtained from 2-[18F]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-[18F]fluoroethyl azide in the presence of copper wire and aqueous trifluoroacetic acid. Subsequent reaction of 2-[18F]fluoroethylamine with benzoyl chloride in the presence of triethylamine provided N-[18F]fluoroethyl benzamide in 63% decay-corrected radiochemical yield from 2-[18F]fluoroethyl azide. The utility of the Cu(0)/H+ azide reduction method was further exemplified by preparation of the potential GABAA tracer 9H-β-carboline N-2-[18F]fluoroethylamide, which was obtained in 46% decay-corrected radiochemical yield by reaction of 2-[18F]fluoroethylamine with the corresponding 9H-β-carboline pentafluorophenyl ester. Copyright © 2012 John Wiley & Sons, Ltd. |
| Databáze: |
OpenAIRE |
| Externí odkaz: |
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