Journal of Radiopharmaceuticals and Molecular Probes (대한방사성의약품학회지)

Korean Society of Radiopharmaceuticals and Molecular Probes (대한방사성의약품학회)
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Recent advances of aromatic C-F bond borylation and its application to positron emission tomography

  • Song, Dalnim (Center for Self-assembly and Complexity, Institute for Basic Science (IBS)) ;
  • Lee, Sanghee (Department of Transdisciplinary Studies, Graduate School of Convergence Science and Technology, Seoul National University) ;
  • Lee, Byung Chul (Department of Nuclear Medicine, Seoul National University Bundang Hospital, Seoul National University College of Medicine) ;
  • Kim, Sang Eun (Department of Transdisciplinary Studies, Graduate School of Convergence Science and Technology, Seoul National University) ;
  • Lee, Eunsung (Center for Self-assembly and Complexity, Institute for Basic Science (IBS))
  • Received : 2015.11.16
  • Accepted : 2015.12.15
  • Published : 2015.12.30
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Abstract

Carbon-fluorine (C-F) bonds have been found ubiquitously in pharmaceuticals, radiopharmaceuticals, agrochemicals, and material science due to their unique properties such as thermal and oxidative stability and lipophilicity to improve bioavailability. For the past five years, there have been significant advances in F-18 fluorination of aromatic complex molecules combined with the development of late-stage fluorination reactions. More recently, direct incorporation of F-18 to fluorinated aromatic molecules via borylation of C-F bonds has been developed by Niwa and Hosoya. In this minireview, we will discuss the progress of C-F bondborylation of fluorinated arenes utilizing transition metal catalysts and the impact on the development of F-18 radiotracers for positron emission tomography (PET).

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