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DOI: 10.1055/s-0033-1340373
[18F]Trifluoromethylation of Aryl and Heteroaryl Iodides
A Broadly Applicable [18F]Trifluoromethylation of Aryl Iodides and Heteroaryl Iodides for PET Imaging.
Nature Chem. 2013;
5: 941-944
Publikationsverlauf
Publikationsdatum:
13. Dezember 2013 (online)
Significance
The authors disclose the easy and broadly applicable late-stage [18F]trifluoromethylation of various aryl and heteroaryl iodides using methyl chlorodifluoroacetate, CuI, TMEDA, and [18F]fluoride. The [18F]trifluoromethylated (hetero)aryls, which serve as [18F]-PET (positron emission tomography) tracers, are obtained in good yields.
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Comment
Usually, access to [18F]-labelled probes is limited by the short half-life of 18F and the small availability of parent 18F sources that show a suitable reactivity, such as [18F]F– and [18F]F2. Furthermore, this operational simple [18F]CuCF3-based strategy excludes the tedious preparation of complex organometallic precursors and may be performed on air. The active [18F]CF3Cu is generated in situ.
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