Automation of the radiosynthesis and purification procedures for [18F]Fluspidine preparation, a new radiotracer for clinical investigations in PET imaging of σ(1) receptors in brain

Appl Radiat Isot. 2014 Feb:84:1-7. doi: 10.1016/j.apradiso.2013.10.015. Epub 2013 Nov 5.

Abstract

The radiosynthesis of [(18)F]Fluspidine, a potent σ1 receptor imaging probe for pre-clinical/clinical studies, was implemented on a TRACERlab(TM) FX F-N synthesizer. [(18)F]2 was synthesized in 15 min at 85 °C starting from its tosylate precursor. Purification via semi-preparative RP-HPLC was investigated using different columns and eluent compositions and was most successful on a polar RP phase with acetonitrile/water buffered with NH4OAc. After solid phase extraction, [(18)F]Fluspidine was formulated and produced within 59±4 min with an overall radiochemical yield of 37±8%, a radiochemical purity of 99.3±0.5% and high specific activity (176.6±52.0 GBq/µmol).

Keywords: One-step automated radiosynthesis; Positron emission tomography; [(18)F]Fluspidine; σ(1) receptors..

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Automation, Laboratory
  • Benzofurans / chemical synthesis*
  • Chromatography, High Pressure Liquid
  • Fluorine Radioisotopes* / chemistry
  • Piperidines / chemical synthesis*
  • Positron-Emission Tomography / methods
  • Radiochemistry / methods
  • Radiopharmaceuticals / chemical synthesis*

Substances

  • 1'-benzyl-3-(2-fluoroethyl)-3H-spiro((2)benzofuran-1,4'-piperidine)
  • Benzofurans
  • Fluorine Radioisotopes
  • Piperidines
  • Radiopharmaceuticals