An efficient synthesis of dopamine transporter tracer [¹⁸F]FECNT

Appl Radiat Isot. 2013 Feb:72:128-32. doi: 10.1016/j.apradiso.2012.10.010. Epub 2012 Oct 23.

Abstract

A simple synthesis of the dopamine transporter ligand [(18)F]FECNT with high radiochemical yield and short synthesis time, suitable for routine production is reported. Reaction of 2β-carbomethoxy-3β-(4-chlorophenyl)nortropane with [(18)F]2-fluoroethyl triflate ([(18)F]FEtOTf) at room temperature for 4 min provided [(18)F]FECNT in 84% decay corrected radiochemical yield. Since [(18)F]FEtOTf was prepared from [(18)F]2-fluoroethyl bromide that was isolated from its starting material, formation of unwanted side products and the amount of expensive precursor used could be greatly reduced. The overall radiochemical yields of [(18)F]FECNT were 40% (n=29) and the total synthesis time was ca. 100 min. The average specific activity of [(18)F]FECNT was 377.4 GBq/μmol (10.2 Ci/μmol).

Publication types

  • Research Support, N.I.H., Extramural

MeSH terms

  • Chromatography, High Pressure Liquid
  • Dopamine Plasma Membrane Transport Proteins / analysis*
  • Fluorine Radioisotopes / chemistry*
  • Nortropanes / chemical synthesis*

Substances

  • 2-carbomethoxy-3-(4-chlorophenyl)-8-(2-fluoroethyl)nortropane
  • Dopamine Plasma Membrane Transport Proteins
  • Fluorine Radioisotopes
  • Nortropanes