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A broadly applicable [18F]trifluoromethylation of aryl and heteroaryl iodides for PET imaging

Huiban, Mickael, Tredwell, Matthew, Mizuta, Satoshi, Wan, Zehong, Zhang, Xiaomin, Collier, Thomas Lee, Gouverneur, Veronique and Passchier, Jan 2013. A broadly applicable [18F]trifluoromethylation of aryl and heteroaryl iodides for PET imaging. Nature Chemistry 5 (11) , pp. 941-944. 10.1038/nchem.1756

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Abstract

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 18F-labelled probes are inaccessible or notoriously difficult to produce. Typical challenges associated with 18F radiochemistry are the short half-life of 18F (<2 h), the use of sub-stoichiometric amounts of 18F, relative to the precursor and other reagents, as well as the limited availability of parent 18F sources of suitable reactivity ([18F]F– and [18F]F2). There is a high-priority demand for general methods allowing access to [18F]CF3-substituted molecules for application in pharmaceutical discovery programmes. We report the development of a process for the late-stage [18F]trifluoromethylation of (hetero)arenes from [18F]fluoride using commercially available reagents and (hetero)aryl iodides. This [18F]CuCF3–based protocol benefits from a large substrate scope and is characterized by its operational simplicity.

Item Type: Article
Date Type: Published Online
Status: Published
Schools: Medicine
Publisher: Nature Publishing Group
ISSN: 1755-4330
Last Modified: 12 Jun 2019 10:55
URI: http://orca.cf.ac.uk/id/eprint/122209

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