Ligand-Enabled Copper-Mediated Radioiodination of Arenes
Holly McErlain, Matthew J. Andrews, Allan J. B. Watson, Sally L. Pimlott, Andrew Sutherland
Abstract
High Resolution Image Download MS PowerPoint Slide The discovery of a copper precatalyst that facilitates the key mechanistic steps of arene halodeboronation has allowed a step change in the synthesis of radioiodine-containing arenes. The active precatalyst [Cu(OAc)(phen) 2 ]OAc was shown to perform room temperature radio-iododeboronation of aryl boronic acids with 1–2 mol % loadings and 10 min reaction times. These mild conditions enable particularly clean reactions, as demonstrated with the efficient preparation of the radiopharmaceutical and SPECT tracer, meta -iodobenzylguanidine (MIBG).
Topics & Concepts
ChemistryLigand (biochemistry)ArylCopperCombinatorial chemistryRadiochemistryOrganic chemistryReceptorBiochemistryAlkylRadiopharmaceutical Chemistry and ApplicationsBoron Compounds in ChemistryPeptidase Inhibition and Analysis