Ligand-enabled copper-mediated radioiodination of arenes

Holly McErlain, Matthew J. Andrews, Allan J. B. Watson, Sally L. Pimlott, Andrew Sutherland

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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).

Original languageEnglish
Number of pages5
JournalOrganic Letters
VolumeAhead of Print
Early online date9 Feb 2024
DOIs
Publication statusE-pub ahead of print - 9 Feb 2024

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