Facile room temperature synthesis of fluorine-18 labeled fluoronicotinic acid-2,3,5,6-tetrafluorophenyl ester without azeotropic drying of fluorine-18.
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.
Imaging Probe Development Center, National Heart, Lung, and Blood Institute, National Institutes of Health, Rockville, MD. Electronic address: bhattacharyyaf@mail.nih.gov.
Falguni
F
Basuli
Imaging Probe Development Center, National Heart, Lung, and Blood Institute, National Institutes of Health, Rockville, MD.
Xiang
X
Zhang
Molecular Imaging Program, National Cancer Institute, National Institutes of Health, Bethesda, MD.
Elaine M
EM
Jagoda
Molecular Imaging Program, National Cancer Institute, National Institutes of Health, Bethesda, MD.
Peter L
PL
Choyke
Imaging Probe Development Center, National Heart, Lung, and Blood Institute, National Institutes of Health, Rockville, MD.
Rolf E
RE
Swenson
D005462:Fluorine Radioisotopes / Q000737:chemistry*; D007553:Isotope Labeling / Q000379:methods*; D009525:Niacin / Q000737:chemistry*; D009539:Nicotinic Acids / Q000737:chemistry*; D013696:Temperature
C547953:6-fluoronicotinic acid 2,3,5,6-tetrafluorophenyl ester; D005462:Fluorine Radioisotopes; D009539:Nicotinic Acids; D009525:Niacin
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