Synthesis procedure for routine production of 2-[18F]fluoro-3-(2(S)-azetidinylmethoxy)pyridine (2-[18F]F-A-85380)

Appl Radiat Isot. 2007 Nov;65(11):1244-8. doi: 10.1016/j.apradiso.2007.02.009. Epub 2007 Mar 12.

Abstract

2-[18F]Fluoro-3-(2(S)-azetidinylmethoxy)pyridine (2-[18F]F-A-85380) was among the first subtype selective radioligands to visualise the in vivo distribution of alpha4beta2-containing neuronal nicotinic acetylcholine receptors (nAChRs) in human brain. We developed a one-pot synthesis for the preparation of 2-[18F]F-A-85380 in a commercially available TRACERlab FXF-N synthesis module. The synthesis comprises a nucleophilic substitution followed by hydrolysis of a t-butyloxycarbonyl (BOC)-protected intermediate. After formulation for intravenous application up to 20 G Bq 2-[18F]F-A-85380 were produced from a starting activity of 100 G Bq [18F]fluoride in 60 min with a specific activity of about 4.10(5)GBq/mmol and a mean radiochemical purity of more than 99%.

MeSH terms

  • Fluorine Radioisotopes*
  • Humans
  • Methods
  • Pyridines / chemical synthesis*
  • Radiopharmaceuticals / chemical synthesis
  • Receptors, Nicotinic / analysis

Substances

  • 2-fluoro-3-(2(S)-azetidinylmethoxy)pyridine
  • Fluorine Radioisotopes
  • Pyridines
  • Radiopharmaceuticals
  • Receptors, Nicotinic