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KMID : 1145520190050020145
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Journal of Radiopharmaceuticals and Molecular Probes
2019 Volume.5 No. 2 p.145 ~ p.151
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Recent progress in aromatic radiofluorination
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Kwon Young-Do
Chun Joong-Hyun
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Abstract
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Fluorine-18 is considered to be the radionuclide of choice for positron emission tomography (PET). Thus, thedevelopment of small molecule-based radiopharmaceuticals for use in diagnostic imaging relies heavily onefficient radiofluorination techniques. Until the early 2000s, diaryliodonium salts and aryliodonium ylides werewidely employed as labeling precursors to yield aromatic PET radiotracers with cyclotron-produced [18F]fluorideion. Rapid recent progress in the development of efficient borylation methods has led to a paradigm shift in18F-labeling methods. In addition, deoxyfluorination has attracted a great deal of interest as an alternativeapproach to aryl ring activation with 18F-. In this review, methods for radiolabel development are discussed witha specific focus on the progress made in the last 5 years. Other interesting 18F-based protocols are also brieflyintroduced. New methods for exploiting 18F- are expected to increase the number of 18F-labeling methods, toallow applications in a range of chemical environments.
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KEYWORD
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Fluorine-18, Deoxyfluorination, Radiofluorination, Radiotracer, PET
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