title: Tos-Nos-Mos: Synthesis of different aryl sulfonate precursors for the radiosynthesis of the alpha7 nicotinic acetylcholine receptor radioligand [(18)F]NS14490.
abstract: Radiopharmacological investigations of [(18)F]NS14490 have proven that this radiotracer could be a potential PET radiotracer for imaging of alpha7 nicotinic acetylcholine receptor particularly with regard to vulnerable plaques of diseased vessels. For further optimisation of the previously automated one-pot radiosynthesis of [(18)F]NS14490 using a tosylate precursor, precursors with other leaving groups (nosylate and mosylate) were synthesized and compared with the tosylate with respect to their reactivities towards [(18)F]fluoride. The use of these different precursors resulted in comparable labelling yields of [(18)F]NS14490. A novel mosylate precursor was synthesized and evaluated, which has revealed a higher stability during a storage period of five months compared to the corresponding tosylate and nosylate.
authors.affiliation: Helmholtz-Zentrum Dresden - Rossendorf, Institute of Radiopharmaceutical Cancer Research, Departments of Neuroradiopharmaceuticals and Radiopharmaceutical and Chemical Biology, POB 51 01 19, D-01314 Dresden, Germany.
authors.forename: Sven
authors.initials: S
authors.lastname: Rötering
authors.affiliation: Helmholtz-Zentrum Dresden - Rossendorf, Institute of Radiopharmaceutical Cancer Research, Departments of Neuroradiopharmaceuticals and Radiopharmaceutical and Chemical Biology, POB 51 01 19, D-01314 Dresden, Germany.
authors.forename: Matthias
authors.initials: M
authors.lastname: Scheunemann
authors.affiliation: Helmholtz-Zentrum Dresden - Rossendorf, Institute of Radiopharmaceutical Cancer Research, Departments of Neuroradiopharmaceuticals and Radiopharmaceutical and Chemical Biology, POB 51 01 19, D-01314 Dresden, Germany.
authors.forename: Robert
authors.initials: R
authors.lastname: Günther
authors.affiliation: Helmholtz-Zentrum Dresden - Rossendorf, Institute of Radiopharmaceutical Cancer Research, Departments of Neuroradiopharmaceuticals and Radiopharmaceutical and Chemical Biology, POB 51 01 19, D-01314 Dresden, Germany.
authors.forename: Reik
authors.initials: R
authors.lastname: Löser
authors.affiliation: Helmholtz-Zentrum Dresden - Rossendorf, Institute of Radiopharmaceutical Cancer Research, Departments of Neuroradiopharmaceuticals and Radiopharmaceutical and Chemical Biology, POB 51 01 19, D-01314 Dresden, Germany.
authors.forename: Achim
authors.initials: A
authors.lastname: Hiller
authors.affiliation: DanPET AB, Rosenstigen 7, SE-216 19 Malmö, Sweden.
authors.lastname: Dan Peters
authors.affiliation: Helmholtz-Zentrum Dresden - Rossendorf, Institute of Radiopharmaceutical Cancer Research, Departments of Neuroradiopharmaceuticals and Radiopharmaceutical and Chemical Biology, POB 51 01 19, D-01314 Dresden, Germany.
authors.forename: Peter
authors.initials: P
authors.lastname: Brust
authors.affiliation: Helmholtz-Zentrum Dresden - Rossendorf, Institute of Radiopharmaceutical Cancer Research, Departments of Neuroradiopharmaceuticals and Radiopharmaceutical and Chemical Biology, POB 51 01 19, D-01314 Dresden, Germany. Electronic address: s.fischer@hzdr.de.
authors.forename: Steffen
authors.initials: S
authors.lastname: Fischer
authors.affiliation: Helmholtz-Zentrum Dresden - Rossendorf, Institute of Radiopharmaceutical Cancer Research, Departments of Neuroradiopharmaceuticals and Radiopharmaceutical and Chemical Biology, POB 51 01 19, D-01314 Dresden, Germany.
authors.forename: Jörg
authors.initials: J
authors.lastname: Steinbach
mesh_terms: D000818:Animals; D001190:Arylsulfonates / Q000737:chemistry; D001557:Benzenesulfonates / Q000138:chemical synthesis / Q000737:chemistry; D004355:Drug Stability; D005462:Fluorine Radioisotopes / Q000737:chemistry; D007211:Indoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000493:pharmacokinetics; D057054:Molecular Imaging; D015394:Molecular Structure; D010069:Oxadiazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000493:pharmacokinetics; D049268:Positron-Emission Tomography; D011869:Radioligand Assay; D019275:Radiopharmaceuticals / Q000138:chemical synthesis* / Q000737:chemistry / Q000493:pharmacokinetics; D014105:Tosyl Compounds / Q000138:chemical synthesis / Q000737:chemistry; D064569:alpha7 Nicotinic Acetylcholine Receptor / Q000378:metabolism*
chemical_list: D001190:Arylsulfonates; D001557:Benzenesulfonates; D005462:Fluorine Radioisotopes; D007211:Indoles; C584300:NS14490; D010069:Oxadiazoles; D019275:Radiopharmaceuticals; D014105:Tosyl Compounds; D064569:alpha7 Nicotinic Acetylcholine Receptor
keywords: Alpha7 nAChR ligand; Mosylate; Nosylate; PET; Reactivity of precursor; Synthesis of precursor; Tosylate