[ super(18)F]CuCF sub(3): A [ super(18)F]Trifluoromethylating Agent for Arylboronic Acids and Aryl Iodides

Positron emission tomography has emerged as the leading method for medical imaging with fluorine-18 as the most widely used radioactive isotope. Here we report a semi-automated method for the preparation of valuable [ super(18)F]trifluoromethylcopper, as well as its use for the radiosynthesis of [ s...

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Veröffentlicht in:Chemistry : a European journal 2014-07, Vol.20 (31), p.9514-9518
Hauptverfasser: Ivashkin, Pavel, Lemonnier, Gerald, Cousin, Jonathan, Gregoire, Vincent, Labar, Daniel, Jubault, Philippe, Pannecoucke, Xavier
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Sprache:eng
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Zusammenfassung:Positron emission tomography has emerged as the leading method for medical imaging with fluorine-18 as the most widely used radioactive isotope. Here we report a semi-automated method for the preparation of valuable [ super(18)F]trifluoromethylcopper, as well as its use for the radiosynthesis of [ super(18)F]trifluoromethylarenes and heteroarenes. Mild conditions of [ super(18)F]trifluoromethylation make this method particularly useful for the radiosynthesis of pharmacologically relevant [ super(18)F]trifluoromethylarenes and heteroarenes. super(18)F Radiochemistry: A semi-automated method for the fast preparation of radiolabelled (trifluoromethyl)copper is reported (see scheme), thus making [ super(18)F]CuCF sub(3) almost as accessible as [ super(18)F]fluoride itself for the preparation of radiolabelled trifluoromethylated probes. It can be used for the preparation of radiolabelled trifluoromethylarenes from arylboronic acids and aryliodides. This methodology is clean, efficient and consistent with the specific requirements of radiochemistry.
ISSN:0947-6539
1521-3765
DOI:10.1002/chem.201403630