Improved automated synthesis of [18F]fluoroethylcholine as a radiotracer for cancer imaging

Bioorg Med Chem. 2007 May 1;15(9):3171-5. doi: 10.1016/j.bmc.2007.02.038. Epub 2007 Feb 22.

Abstract

[(18)F]Fluoroethylcholine has been recently introduced as a promising (18)F-labelled analogue of [(11)C]choline which had been previously described as a tracer for metabolic cancer imaging with positron emission tomography (PET). Due to the practical advantages of using the longer-lived radioisotope (18)F (t(1/2)=110 min), offering the opportunity of a more widespread clinical application, we established a reliable, fully automated synthesis for its production using a modified, commercially available module. [(18)F]Fluoroethylcholine was prepared from N,N-dimethylaminoethanol by iodide catalyzed alkylation with 1-[(18)F]fluoro-2-tosylethane as alkylating agent, resulting in a total radiochemical yield of 30+/-6% after a synthesis time of 50 min. The specific activity of [(18)F]fluoroethylcholine was >55 GBq/micromol and the radiochemical purity 95-99%.

MeSH terms

  • Choline / analogs & derivatives*
  • Choline / chemical synthesis
  • Choline / chemistry
  • Chromatography, High Pressure Liquid / instrumentation
  • Chromatography, High Pressure Liquid / methods
  • Fluorine Radioisotopes
  • Molecular Structure
  • Neoplasms / diagnosis*
  • Sensitivity and Specificity

Substances

  • Fluorine Radioisotopes
  • fluoroethylcholine
  • Choline