title: Two-step radiosynthesis of 18)F]FE-β-CIT and [18F]PR04.MZ.
abstract: The cocaine-derived dopamine reuptake inhibitors FE-β-CIT (8-(2-fluoroethyl)-3-(4-iodophenyl)-8-azabicyclo[3.2.1]octane-2-carboxylic acid methyl ester) (1) and PR04.MZ(8-(4-fluorobut-2-ynyl)-3-p-tolyl-8-azabicyclo[3.2.1]octane-2-carboxylic acid methyl ester) (2) were labelled with (18)F-fluorine using a two-step route. 2-[(18)F]Fluoroethyltosylate and 4-[(18)F]fluorobut-2-yne-1-yl tosylate were used as labelling reagents, respectively. Radiochemically pure (>98%) [(18)F]FE-β-CIT and [(18)F]PRD04.MZ (32-86 GBq/µmol) were obtained after a synthesis time of 100 min in about 25% non-decay-corrected overall yield.
authors.affiliation: Institut für Kernchemie, Universität Mainz, Fritz Strassmann Weg 2, 55128, Mainz, Germany; Department of Chemistry, UiO Postboks 1033 - Blindern, 0315, Oslo, Norge.
authors.forename: Patrick J
authors.initials: PJ
authors.lastname: Riss
authors.forename: Sabine
authors.initials: S
authors.lastname: Hoehnemann
authors.forename: Markus
authors.initials: M
authors.lastname: Piel
authors.forename: Frank
authors.initials: F
authors.lastname: Roesch
mesh_terms: D060326:Chemistry Techniques, Synthetic / Q000379:methods; D003042:Cocaine / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry; D005462:Fluorine Radioisotopes / Q000737:chemistry*; D007553:Isotope Labeling / Q000379:methods; D019275:Radiopharmaceuticals / Q000138:chemical synthesis*; D014326:Tropanes / Q000138:chemical synthesis*
chemical_list: C000589729:8-(2-fluoroethyl)-3-(4-iodophenyl)-8-azabicyclo(3.2.1)octane-2-carboxylic acid methyl ester; D005462:Fluorine Radioisotopes; C545366:PR04.MZ compound; D019275:Radiopharmaceuticals; D014326:Tropanes; D003042:Cocaine
keywords: automated synthesis; dopamine transporter; fluorine-18; tropanes