title: A fully automated radiosynthesis of [18F]fluoroethyl-diprenorphine on a single module by use of SPE cartridges for preparation of high quality 2-[18F]fluoroethyl tosylate.
abstract: We have developed a new method for automated production of 2-[18F]fluoroethyl tosylate ([18F]FETos) that enables 18F-alkylation to provide PET tracers with high chemical purity. The method is based on the removal of excess ethylene glycol bistosylate precursor by precipitation and subsequent filtration and purification of the filtrate by means of solid phase extraction cartridges (SPE). The method is integrated to a single synthesis module and thereby provides the advantage over previous methods of not requiring HPLC purification, as demonstrated by the full radiosynthesis of the potent opioid receptor PET tracer [18F]fluoroethyldiprenorphine.
authors.affiliation: Department of Chemistry, University of Oslo, PO Box 1033, Blindern, N-0315 Oslo, Norway. b.w.schoultz@kjemi.uio.no
authors.forename: Bent W
authors.initials: BW
authors.lastname: Schoultz
authors.forename: Brian J
authors.initials: BJ
authors.lastname: Reed
authors.forename: János
authors.initials: J
authors.lastname: Marton
authors.forename: Frode
authors.initials: F
authors.lastname: Willoch
authors.forename: Gjermund
authors.initials: G
authors.lastname: Henriksen
mesh_terms: D057205:Automation, Laboratory; D001557:Benzenesulfonates / Q000138:chemical synthesis* / Q000737:chemistry / Q000302:isolation & purification; D004174:Diprenorphine / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry / Q000302:isolation & purification; D005462:Fluorine Radioisotopes / Q000737:chemistry*; D007553:Isotope Labeling; D049268:Positron-Emission Tomography; D011786:Quality Control; D019275:Radiopharmaceuticals / Q000138:chemical synthesis* / Q000737:chemistry / Q000302:isolation & purification; D052616:Solid Phase Extraction / Q000379:methods* / Q000592:standards
chemical_list: D001557:Benzenesulfonates; D005462:Fluorine Radioisotopes; D019275:Radiopharmaceuticals; C000590219:fluoroethyl tosylate; D004174:Diprenorphine