Enhanced copper-mediated (18)F-fluorination of aryl boronic esters provides eight radiotracers for PET applications

Chem Commun (Camb). 2016 Jun 28;52(54):8361-4. doi: 10.1039/c6cc03295h.

Abstract

[(18)F]FMTEB, [(18)F]FPEB, [(18)F]flumazenil, [(18)F]DAA1106, [(18)F]MFBG, [(18)F]FDOPA, [(18)F]FMT and [(18)F]FDA are prepared from the corresponding arylboronic esters and [(18)F]KF/K222 in the presence of Cu(OTf)2py4. The method was successfully applied using three radiosynthetic platforms, and up to 26 GBq of non-carrier added starting activity of (18)F-fluoride.

MeSH terms

  • Boronic Acids / chemistry*
  • Catalysis
  • Copper / chemistry*
  • Esters / chemistry*
  • Fluorine Radioisotopes*
  • Halogenation*
  • Positron-Emission Tomography*
  • Radioactive Tracers

Substances

  • Boronic Acids
  • Esters
  • Fluorine Radioisotopes
  • Radioactive Tracers
  • Copper