Ultrafast Click Chemistry with Fluorosydnones

  • Hui Liu
    Service de Chimie Bio-organique et Marquage (SCBM), IBITECS, CEA Université Paris-Saclay 91191 Gif-sur-Yvette France
  • Davide Audisio
    Service de Chimie Bio-organique et Marquage (SCBM), IBITECS, CEA Université Paris-Saclay 91191 Gif-sur-Yvette France
  • Lucie Plougastel
    Service de Chimie Bio-organique et Marquage (SCBM), IBITECS, CEA Université Paris-Saclay 91191 Gif-sur-Yvette France
  • Elodie Decuypere
    Service de Chimie Bio-organique et Marquage (SCBM), IBITECS, CEA Université Paris-Saclay 91191 Gif-sur-Yvette France
  • David‐Alexandre Buisson
    Service de Chimie Bio-organique et Marquage (SCBM), IBITECS, CEA Université Paris-Saclay 91191 Gif-sur-Yvette France
  • Oleksandr Koniev
    Syndivia SAS 650 Boulevard Gonthier O'Andernach 67400 Illkirch France
  • Sergii Kolodych
    Syndivia SAS 650 Boulevard Gonthier O'Andernach 67400 Illkirch France
  • Alain Wagner
    Laboratory of Functional Chemo-Systems UMR 7199 CNRS-UdS 67401 Illkirch France
  • Mourad Elhabiri
    Laboratory of Bioorganic and Medicinal Chemistry, UMR 7509 CNRS ECPM 25, rue Becquerel 67200 Strasbourg France
  • Anna Krzyczmonik
    Turku PET Centre and Department of Chemistry University of Turku 20520 Turku Finland
  • Sarita Forsback
    Turku PET Centre and Department of Chemistry University of Turku 20520 Turku Finland
  • Olof Solin
    Turku PET Centre and Department of Chemistry University of Turku 20520 Turku Finland
  • Véronique Gouverneur
    Chemistry Research Laboratory University of Oxford 12 Mansfield Road Oxford OX1 3TA UK
  • Frédéric Taran
    Service de Chimie Bio-organique et Marquage (SCBM), IBITECS, CEA Université Paris-Saclay 91191 Gif-sur-Yvette France

書誌事項

公開日
2016-08-25
権利情報
  • http://onlinelibrary.wiley.com/termsAndConditions#vor
DOI
  • 10.1002/anie.201606495
公開者
Wiley

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説明

<jats:title>Abstract</jats:title><jats:p>We report the synthesis and reactivity of 4‐fluorosydnones, a unique class of mesoionic dipoles displaying exquisite reactivity towards both copper‐catalyzed and strain‐promoted cycloaddition reactions with alkynes. Synthetic access to these new mesoionic compounds was granted by electrophilic fluorination of σ‐sydnone Pd<jats:sup>II</jats:sup> precursors in the presence of Selectfluor. Their reactions with terminal and cyclic alkynes were found to proceed very rapidly and selectively, affording 5‐fluoro‐1,4‐pyrazoles with bimolecular rate constants up to 10<jats:sup>4</jats:sup> <jats:sc>m</jats:sc><jats:sup>−1</jats:sup> s<jats:sup>−1</jats:sup>, surpassing those documented in the literature with cycloalkynes. Kinetic studies were carried out to unravel the mechanism of the reaction, and the value of 4‐fluorosydnones was further highlighted by successful radiolabeling with [<jats:sup>18</jats:sup>F]Selectfluor.</jats:p>

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