Ligand-Enabled Copper-Mediated Radioiodination of Arenes.

ABSTRACT: 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).

SUBMITTER: McErlain H 

PROVIDER: S-EPMC10897930 | biostudies-literature | 2024 Feb

REPOSITORIES: biostudies-literature