A. A. Cant, S. Champion, R. Bhalla, S. L. Pimlott, A. Sutherland
1521-3773 (Electronic) 1433-7851 (Linking)
Angew Chem Int Ed Engl
WestCHEM, School of Chemistry, University of Glasgow, G12 8QQ, Glasgow, UK.
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).