A Fluoride-Derived Electrophilic Late-Stage Fluorination Reagent for PET Imaging

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A Fluoride-Derived Electrophilic Late-Stage Fluorination Reagent for PET Imaging

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Title: A Fluoride-Derived Electrophilic Late-Stage Fluorination Reagent for PET Imaging
Author: Lee, Eunsung; Kamlet, Adam Seth; Powers, David C.; Neumann, Constanze Nicole; Boursalian, Gregory Bagrad; Furuya, Takeru; Choi, Daniel C.; Ritter, Tobias; Hooker, Jacob M.

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Citation: Lee, Eunsung, Adam Seth Kamlet, David C. Powers, Constanze Nicole Neumann, Gregory Bagrad Boursalian, Takeru Furuya, Daniel C. Choi, Jacob M. Hooker, and Tobias Ritter. 2011. A fluoride-derived electrophilic late-stage fluorination reagent for PET imaging. Science 334(6056): 639-642.
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Abstract: The unnatural isotope fluorine-18 \((^{18}F)\) is used as a positron emitter in molecular imaging. Currently, many potentially useful \(^{18}F\)-labeled probe molecules are inaccessible for imaging because no fluorination chemistry is available to make them. The 110-minute half-life of \(^{18}F\) requires rapid syntheses for which \([^{18}F]\)fluoride is the preferred source of fluorine because of its practical access and suitable isotope enrichment. However, conventional \([^{18}F]\)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 \(^{18}F\)-labeled molecules via late-stage fluorination. Late-stage fluorination enables the synthesis of conventionally unavailable positron emission tomography (PET) tracers for anticipated applications in pharmaceutical development as well as preclinical and clinical PET imaging.
Published Version: doi:10.1126/science.1212625
Other Sources: http://www.ncbi.nlm.nih.gov/pubmed/22053044
Terms of Use: This article is made available under the terms and conditions applicable to Open Access Policy Articles, as set forth at http://nrs.harvard.edu/urn-3:HUL.InstRepos:dash.current.terms-of-use#OAP
Citable link to this page: http://nrs.harvard.edu/urn-3:HUL.InstRepos:8187682
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