title: Enhanced copper-mediated (18)F-fluorination of aryl boronic esters provides eight radiotracers for PET applications.
abstract: [(18)F]FMTEB, [(18)F]FPEB, [(18)F]flumazenil, [(18)F]DAA1106, [(18)F]MFBG, [(18)F]FDOPA, [(18)F]FMT and [(18)F]FDA are prepared from the corresponding arylboronic esters and [(18)F]KF/K222 in the presence of Cu(OTf)2py4. The method was successfully applied using three radiosynthetic platforms, and up to 26 GBq of non-carrier added starting activity of (18)F-fluoride.
authors.affiliation: University of Oxford, Chemistry Research Laboratory, 12 Mansfield Road, OX1 3TA Oxford, UK. veronique.gouverneur@chem.ox.ac.uk.
authors.forename: Sean
authors.initials: S
authors.lastname: Preshlock
authors.affiliation: University of Oxford, Chemistry Research Laboratory, 12 Mansfield Road, OX1 3TA Oxford, UK. veronique.gouverneur@chem.ox.ac.uk.
authors.forename: Samuel
authors.initials: S
authors.lastname: Calderwood
authors.affiliation: University of Oxford, Chemistry Research Laboratory, 12 Mansfield Road, OX1 3TA Oxford, UK. veronique.gouverneur@chem.ox.ac.uk.
authors.forename: Stefan
authors.initials: S
authors.lastname: Verhoog
authors.affiliation: University of Oxford, Chemistry Research Laboratory, 12 Mansfield Road, OX1 3TA Oxford, UK. veronique.gouverneur@chem.ox.ac.uk.
authors.forename: Matthew
authors.initials: M
authors.lastname: Tredwell
authors.affiliation: Imanova, Burlington Danes building Imperial College, London Hammersmith Hospital, Du Cane Road, London W12 0NN, UK.
authors.forename: Mickael
authors.initials: M
authors.lastname: Huiban
authors.affiliation: ABX GmbH Heinrich-Glaeser-Strasse 10-14, D-01454 Radeberg, Germany.
authors.forename: Antje
authors.initials: A
authors.lastname: Hienzsch
authors.affiliation: University of Oxford, Chemistry Research Laboratory, 12 Mansfield Road, OX1 3TA Oxford, UK. veronique.gouverneur@chem.ox.ac.uk.
authors.forename: Stefan
authors.initials: S
authors.lastname: Gruber
authors.affiliation: University of Oxford, Chemistry Research Laboratory, 12 Mansfield Road, OX1 3TA Oxford, UK. veronique.gouverneur@chem.ox.ac.uk.
authors.forename: Thomas C
authors.initials: TC
authors.lastname: Wilson
authors.affiliation: University of Oxford, Chemistry Research Laboratory, 12 Mansfield Road, OX1 3TA Oxford, UK. veronique.gouverneur@chem.ox.ac.uk.
authors.forename: Nicholas J
authors.initials: NJ
authors.lastname: Taylor
authors.affiliation: University of Oxford, Chemistry Research Laboratory, 12 Mansfield Road, OX1 3TA Oxford, UK. veronique.gouverneur@chem.ox.ac.uk and Normandie University, UNICAEN, CERMN, F-14032 Caen, France.
authors.forename: Thomas
authors.initials: T
authors.lastname: Cailly
authors.affiliation: University of Oxford, Chemistry Research Laboratory, 12 Mansfield Road, OX1 3TA Oxford, UK. veronique.gouverneur@chem.ox.ac.uk.
authors.forename: Michael
authors.initials: M
authors.lastname: Schedler
authors.affiliation: Advion BioSystems, 10 Brown Road, Suite 101, Ithaca, NY 14850, USA.
authors.forename: Thomas Lee
authors.initials: TL
authors.lastname: Collier
authors.affiliation: Imanova, Burlington Danes building Imperial College, London Hammersmith Hospital, Du Cane Road, London W12 0NN, UK.
authors.forename: Jan
authors.initials: J
authors.lastname: Passchier
authors.affiliation: ABX GmbH Heinrich-Glaeser-Strasse 10-14, D-01454 Radeberg, Germany.
authors.forename: René
authors.initials: R
authors.lastname: Smits
authors.affiliation: ABX GmbH Heinrich-Glaeser-Strasse 10-14, D-01454 Radeberg, Germany.
authors.forename: Jan
authors.initials: J
authors.lastname: Mollitor
authors.affiliation: ABX GmbH Heinrich-Glaeser-Strasse 10-14, D-01454 Radeberg, Germany.
authors.forename: Alexander
authors.initials: A
authors.lastname: Hoepping
authors.affiliation: ABX GmbH Heinrich-Glaeser-Strasse 10-14, D-01454 Radeberg, Germany.
authors.forename: Marco
authors.initials: M
authors.lastname: Mueller
authors.affiliation: Global Chemistry, UCB New Medicines, UCB Biopharma sprl, 1420 Braine-L'Alleud, Belgium.
authors.forename: Christophe
authors.initials: C
authors.lastname: Genicot
authors.affiliation: Global Chemistry, UCB New Medicines, UCB Biopharma sprl, 1420 Braine-L'Alleud, Belgium.
authors.forename: Joël
authors.initials: J
authors.lastname: Mercier
authors.affiliation: University of Oxford, Chemistry Research Laboratory, 12 Mansfield Road, OX1 3TA Oxford, UK. veronique.gouverneur@chem.ox.ac.uk.
authors.forename: Véronique
authors.initials: V
authors.lastname: Gouverneur
mesh_terms: D001897:Boronic Acids / Q000737:chemistry*; D002384:Catalysis; D003300:Copper / Q000737:chemistry*; D004952:Esters / Q000737:chemistry*; D005462:Fluorine Radioisotopes; D054879:Halogenation; D049268:Positron-Emission Tomography; D011849:Radioactive Tracers
chemical_list: D001897:Boronic Acids; D004952:Esters; D005462:Fluorine Radioisotopes; D011849:Radioactive Tracers; D003300:Copper