Improved synthesis of some commonly used PET radioligands by the use of [11C]methyl triflate

Nucl Med Biol. 1995 Feb;22(2):235-9. doi: 10.1016/0969-8051(94)00083-v.

Abstract

[11C]Methyl triflate was compared with [11C]methyl iodide as a labelled precursor in the synthesis of some commonly used PET radioligands, L-[11C]deprenyl, [11C]m-hydroxyephedrine (MHED), [11C] beta-CIT, [11C] beta-CFT and [11C]SCH 39166 which have been prepared previously in comparatively low yields from [11C]methyl iodide. A new dopamine reuptake radioligand, [11C] alpha-CIT, was also prepared. The results demonstrate that higher yields are obtained with shorter reaction times, lower reaction temperatures and smaller amounts of precursors with [11C]methyl triflate.

Publication types

  • Comparative Study
  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Benzazepines / chemical synthesis*
  • Carbon Radioisotopes*
  • Chromatography, High Pressure Liquid
  • Cocaine / analogs & derivatives
  • Cocaine / chemical synthesis
  • Dopamine Antagonists / chemical synthesis
  • Ephedrine / analogs & derivatives*
  • Ephedrine / chemical synthesis
  • Hydrocarbons, Iodinated
  • Indicators and Reagents
  • Isotope Labeling / methods
  • Magnetic Resonance Spectroscopy
  • Mesylates*
  • Radioligand Assay
  • Selegiline / chemical synthesis*
  • Tomography, Emission-Computed / methods*

Substances

  • Benzazepines
  • Carbon Radioisotopes
  • Dopamine Antagonists
  • Hydrocarbons, Iodinated
  • Indicators and Reagents
  • Mesylates
  • ecopipam
  • Selegiline
  • 3-hydroxyephedrine
  • methyl triflate
  • 2beta-carbomethoxy-3beta-(4-iodophenyl)tropane
  • methyl iodide
  • Ephedrine
  • Cocaine