Ligand-Enabled Copper-Mediated Radioiodination of Arenes.
- Resource Type
- Academic Journal
- Authors
- McErlain H; School of Chemistry, University of Glasgow, Glasgow, G12 8QQ, U.K.; Andrews MJ; EaStCHEM, School of Chemistry, University of St Andrews, North Haugh, St Andrews, Fife KY16 9ST, U.K.; Watson AJB; EaStCHEM, School of Chemistry, University of St Andrews, North Haugh, St Andrews, Fife KY16 9ST, U.K.; Pimlott SL; West of Scotland PET Centre, Greater Glasgow and Clyde NHS Trust, Glasgow, G12 OYN, U.K.; Sutherland A; School of Chemistry, University of Glasgow, Glasgow, G12 8QQ, U.K.
- Source
- Publisher: American Chemical Society Country of Publication: United States NLM ID: 100890393 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1523-7052 (Electronic) Linking ISSN: 15237052 NLM ISO Abbreviation: Org Lett Subsets: PubMed not MEDLINE; MEDLINE
- Subject
- Language
- English
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).