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

Lee, E., Kamlet, A. S., Powers, D. C., Neumann, C. N., Boursalian, G. B., Furuya, T., et al. (2011). A Fluoride-Derived Electrophilic Late-Stage Fluorination Reagent for PET Imaging. Science, 334(6056), 639-642. doi:10.1126/science.1212625.

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 Creators:
Lee, Eunsung1, Author
Kamlet, Adam S.1, Author
Powers, David C.1, Author
Neumann, Constanze N.1, Author              
Boursalian, Gregory B.1, Author              
Furuya, Takeru1, Author
Choi, Daniel C.1, Author
Hooker, Jacob M.2, 3, Author
Ritter, Tobias1, 3, Author              
Affiliations:
1Department for Chemistry and Chemical Biology, Harvard University, 12 Oxford Street, Cambridge, Massachusetts 02138, USA, ou_persistent22              
2Athinoula A. Martinos Center for Biomedical Imaging, Massachusetts General Hospital and Harvard Medical School, Charlestown, MA 02129, USA, ou_persistent22              
3Division of Nuclear Medicine and Molecular Imaging, Department of Radiology, Massachusetts General Hospital, Boston, MA 02114, USA, ou_persistent22              

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 Abstract: 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 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.

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Language(s): eng - English
 Dates: 2011-08-152011-09-132011-11-04
 Publication Status: Published in print
 Pages: 4
 Publishing info: -
 Table of Contents: -
 Rev. Type: Peer
 Identifiers: DOI: 10.1126/science.1212625
 Degree: -

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Title: Science
  Abbreviation : Science
Source Genre: Journal
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Publ. Info: Washington, D.C. : American Association for the Advancement of Science
Pages: - Volume / Issue: 334 (6056) Sequence Number: - Start / End Page: 639 - 642 Identifier: ISSN: 0036-8075
CoNE: https://pure.mpg.de/cone/journals/resource/991042748276600_1