Journal
NATURE CHEMISTRY
Volume 5, Issue 11, Pages 941-944Publisher
NATURE PUBLISHING GROUP
DOI: 10.1038/NCHEM.1756
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Funding
- Imanova
- GlaxoSmithKline
- European Union [PIIF-GA-20100274903]
- Engineering and Physical Sciences Research Council
- Cancer Research UK
- Royal Society
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Molecules labelled with the unnatural isotope fluorine-18 are used for positron emission tomography. Currently, this molecular imaging technology is not exploited at its full potential because many F-18-labelled probes are inaccessible or notoriously difficult to produce. Typical challenges associated with F-18 radiochemistry are the short half-life of F-18 (<2 h), the use of sub-stoichiometric amounts of F-18, relative to the precursor and other reagents, as well as the limited availability of parent F-18 sources of suitable reactivity ([F-18]F- and [F-18]F-2). There is a high-priority demand for general methods allowing access to [F-18]CF3-substituted molecules for application in pharmaceutical discovery programmes. We report the development of a process for the late-stage [F-18]trifluoromethylation of (hetero)arenes from [F-18]fluoride using commercially available reagents and (hetero) aryl iodides. This [F-18]CuCF3-based protocol benefits from a large substrate scope and is characterized by its operational simplicity.
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