A Fluoride-Derived Electrophilic Late-Stage Fluorination Reagent for PET Imaging
- Lee, E.
- Kamlet, A.
- Powers, D.
- Neumann, C.
- Boursalian, G.
- Furuya, T.
- Choi, D.
- Hooker, J.
- Ritter, T.
DOIAbstract
The unnatural isotope fluorine-18 (18F) is used as a positron emitter in molecular imaging. Currently, many potentially useful 18F-labeled probe molecules are inaccessible for imaging because no fluorination chemistry is available to make them. The 110-minute half-life of 18F requires rapid syntheses for which [18F]fluoride is the preferred source of fluorine because of its practical access and suitable isotope enrichment. However, conventional [18F]fluoride chemistry has been limited to nucleophilic fluorination reactions. We report the development of a palladium-based electrophilic fluorination reagent derived from fluoride and its application to the synthesis of aromatic 18F-labeled molecules via late-stage fluorination. Late-stage fluor...
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