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Tandem Iridium-Catalyzed C–H Borylation/Copper-Mediated Radiofluorination of Aromatic C–H Bonds with [18F]TBAF

  • Maria Morales,
  • Sean Preshlock,
  • Liam S. Sharninghausen,
  • Jay S. Wright,
  • Allen F. Brooks,
  • Melanie S. Sanford,
  • Peter J. H. Scott

摘要

Direct C–H functionalization of (hetero)aromatic C–H bonds with iridium-catalyzed borylation followed by copper-mediated radiofluorination of the in situ generated organoboronates affords fluorine-18 labeled aromatics in high radiochemical conversions and meta-selectivities. This protocol describes the benchtop reaction assembly of the C–H borylation and radiofluorination steps, which can be utilized for the fluorine-18 labeling of densely functionalized bioactive scaffolds.