title: 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.
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).
authors.affiliation: Helmholtz-Zentrum Dresden-Rossendorf, Institute of Radiopharmaceutical Cancer Research(1), Research Site Leipzig, Department of Neuroradiopharmaceuticals, Germany. Electronic address: aurelie.maisonial@inserm.fr.
authors.forename: Aurélie
authors.initials: A
authors.lastname: Maisonial-Besset
authors.affiliation: Helmholtz-Zentrum Dresden-Rossendorf, Institute of Radiopharmaceutical Cancer Research(1), Research Site Leipzig, Department of Neuroradiopharmaceuticals, Germany.
authors.forename: Uta
authors.initials: U
authors.lastname: Funke
authors.affiliation: Helmholtz-Zentrum Dresden-Rossendorf, Institute of Radiopharmaceutical Cancer Research(1), Research Site Leipzig, Department of Neuroradiopharmaceuticals, Germany.
authors.forename: Barbara
authors.initials: B
authors.lastname: Wenzel
authors.affiliation: Helmholtz-Zentrum Dresden-Rossendorf, Institute of Radiopharmaceutical Cancer Research(1), Research Site Leipzig, Department of Neuroradiopharmaceuticals, Germany.
authors.forename: Steffen
authors.initials: S
authors.lastname: Fischer
authors.affiliation: Department of Pharmaceutical and Medicinal Chemistry, University of Münster, Germany.
authors.forename: Katharina
authors.initials: K
authors.lastname: Holl
authors.affiliation: Department of Pharmaceutical and Medicinal Chemistry, University of Münster, Germany.
authors.forename: Bernhard
authors.initials: B
authors.lastname: Wünsch
authors.affiliation: Helmholtz-Zentrum Dresden-Rossendorf, Institute of Radiopharmaceutical Cancer Research(1), Research Site Leipzig, Department of Neuroradiopharmaceuticals, Germany.
authors.forename: Jörg
authors.initials: J
authors.lastname: Steinbach
authors.affiliation: Helmholtz-Zentrum Dresden-Rossendorf, Institute of Radiopharmaceutical Cancer Research(1), Research Site Leipzig, Department of Neuroradiopharmaceuticals, Germany.
authors.forename: Peter
authors.initials: P
authors.lastname: Brust
mesh_terms: D057205:Automation, Laboratory; D001572:Benzofurans / Q000138:chemical synthesis*; D002851:Chromatography, High Pressure Liquid; D005462:Fluorine Radioisotopes / Q000737:chemistry; D010880:Piperidines / Q000138:chemical synthesis*; D049268:Positron-Emission Tomography / Q000379:methods; D011854:Radiochemistry / Q000379:methods; D019275:Radiopharmaceuticals / Q000138:chemical synthesis*
chemical_list: C558383:1'-benzyl-3-(2-fluoroethyl)-3H-spiro((2)benzofuran-1,4'-piperidine); D001572:Benzofurans; D005462:Fluorine Radioisotopes; D010880:Piperidines; D019275:Radiopharmaceuticals
keywords: One-step automated radiosynthesis; Positron emission tomography; [(18)F]Fluspidine; σ(1) receptors.