title: Nickel-mediated radioiodination of aryl and heteroaryl bromides: rapid synthesis of tracers for SPECT imaging.
abstract: Rapid and efficient radioiodination of aryl and heteroaryl bromides has been achieved using a nickel(0)-mediated halogen-exchange reaction. This transformation gives direct access to [(123)I]- and [(125)I]-imaging agents for single photon emission computed tomography (SPECT), such as 5-[(123)I]-A85380 (see scheme, Boc = tert-butyloxycarbonyl, cod = 1,5-cyclooctadiene, TFA = trifluoroacetic acid).
authors.affiliation: WestCHEM, School of Chemistry, University of Glasgow, G12 8QQ, Glasgow, UK.
authors.forename: Alastair A
authors.initials: AA
authors.lastname: Cant
authors.forename: Sue
authors.initials: S
authors.lastname: Champion
authors.forename: Rajiv
authors.initials: R
authors.lastname: Bhalla
authors.forename: Sally L
authors.initials: SL
authors.lastname: Pimlott
authors.forename: Andrew
authors.initials: A
authors.lastname: Sutherland
mesh_terms: D001965:Bromides / Q000737:chemistry*; D003952:Diagnostic Imaging; D006571:Heterocyclic Compounds / Q000737:chemistry*; D007457:Iodine Radioisotopes; D015394:Molecular Structure; D009474:Neurons / Q000166:cytology / Q000378:metabolism*; D009532:Nickel / Q000737:chemistry*; D011978:Receptors, Nicotinic / Q000378:metabolism*; D015899:Tomography, Emission-Computed, Single-Photon
chemical_list: D001965:Bromides; D006571:Heterocyclic Compounds; D007457:Iodine Radioisotopes; D011978:Receptors, Nicotinic; C403531:nicotinic receptor alpha4beta2; D009532:Nickel
keywords: aryl bromides; halogen exchange; imaging agents; nickel; radioiodination