Synthesis of [18F]fluoroetanidazole: a potential new tracer for imaging hypoxia

Nucl Med Biol. 1997 Nov;24(8):755-60. doi: 10.1016/s0969-8051(97)00135-2.

Abstract

A method has been developed for the synthesis of [18F]fluoroetanidazole, a potential tracer for imaging hypoxia with positron emission tomography. The compound is prepared by an active ester coupling reaction between the 2,3,5,6-tetrafluorophenyl ester of 2-nitroimidazole acetic acid and [18F]fluoroethylamine. [18F]Fluoroethylamine is prepared from N-[2-(toluene-4-sulfonyloxy)-ethyl]-phthalimide and [18F]fluoride and purified by distillation. The overall reaction takes about 90 min and gives a yield, uncorrected, of about 25%. Purification on a reversed-phase column is straightforward.

Publication types

  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Etanidazole / analogs & derivatives*
  • Etanidazole / chemical synthesis
  • Etanidazole / chemistry*
  • Fluorine Radioisotopes / chemistry*
  • Hypoxia / diagnostic imaging
  • Isotope Labeling
  • Radiation-Sensitizing Agents / chemistry*
  • Radiopharmaceuticals / chemical synthesis*
  • Tomography, Emission-Computed

Substances

  • Fluorine Radioisotopes
  • Radiation-Sensitizing Agents
  • Radiopharmaceuticals
  • fluoroetanidazole
  • Etanidazole