Radiosynthesis of novel N-18 F-labeled 18 F-FHex-α-l-Glu and 18 F-FHex-β-Glu

J Labelled Comp Radiopharm. 2020 May 15;63(5):222-230. doi: 10.1002/jlcr.3834. Epub 2020 Mar 30.

Abstract

N-18 F-labeled amino acids are important substitutes for new positron emission tomography (PET) imaging tracers complementing the deficiency of 18 F-fluorodeoxyglucose (18 F-FDG). In this work, two novel N-6-18 F-alkyl amino acid imaging agents, 18 F-FHex-α-l-Glu and 18 F-FHex-β-Glu, were designed and synthesized as potential probes for PET imaging of tumors. 18 F-FHex-α-l-Glu was synthesized using the precursor 6 from 18 F-F- with the yield of 16 ± 4% (n = 5, uncorrected) within about 50 minutes. The specific activity was 14.5 GBq/μmol, and the radiochemical purity was more than 95%. 18 F-FHex-β-Glu was synthesized using the precursor 12 based on 18 F-F- with the yield of 11 ± 3% (n = 3, uncorrected) in about 60 minutes. The specific activity was 9.1 GBq/μmol, and the radiochemical purity was more than 95%.

Keywords: 18F-FHex-α-l-Glu; 18F-FHex-β-Glu; alkyl amino acid tracer; radiosynthesis.

MeSH terms

  • Chemistry Techniques, Synthetic / methods
  • Fluorine Radioisotopes* / chemistry
  • Positron-Emission Tomography / methods
  • Radiochemistry / methods
  • Radiopharmaceuticals* / chemical synthesis
  • Radiopharmaceuticals* / chemistry

Substances

  • Fluorine Radioisotopes
  • Radiopharmaceuticals
  • Fluorine-18