Facile room temperature synthesis of fluorine-18 labeled fluoronicotinic acid-2,3,5,6-tetrafluorophenyl ester without azeotropic drying of fluorine-18

Nucl Med Biol. 2016 Dec;43(12):770-772. doi: 10.1016/j.nucmedbio.2016.08.008. Epub 2016 Aug 30.

Abstract

Fluorine-18 labeled fluoronicotinic acid-2,3,5,6-tetrafluorophenyl ester has been successfully synthesized in an unprecedented way by flowing an acetonitrile solution of its quaternary ammonium salt precursor (N,N,N-trimethyl-5-((2,3,5,6-tetrafluorophenoxy)carbonyl)pyridin-2-aminium trifluoromethanesulfonate, 1) through an anion exchange cartridge. The fluorination reaction proceeded at room temperature without azeotropic drying of the fluoride. Over 75% conversion was observed with 10mg of precursor in 2:8, acetonitrile: t-butanol in 1min. The total synthesis time was 5min which is ~30min shorter than the current literature method.

MeSH terms

  • Fluorine Radioisotopes / chemistry*
  • Isotope Labeling / methods*
  • Niacin / chemistry*
  • Nicotinic Acids / chemistry*
  • Temperature*

Substances

  • 6-fluoronicotinic acid 2,3,5,6-tetrafluorophenyl ester
  • Fluorine Radioisotopes
  • Nicotinic Acids
  • Niacin