Base-Mediated Radio-Iodination of Arenes by Using Organosilane and Organogermane as Radiolabelling Precursors.
Hugo BlouxAmit DahiyaAlexandra HébertFrederic FabisFranziska SchoenebeckThomas CaillyPublished in: Chemistry (Weinheim an der Bergstrasse, Germany) (2023)
The radio-iodination of arenes is investigated from organosilane and organogermane precursors using ipso-electrophilic halogenation (IEH). Discovery of a mild base mediated process allows radio-iodination in HFIP (1,1,1,3,3,3-hexafluoro-2-propanol) of either aryl silane or germane, with germanes being more reactive. Clinical potential of arylgermanes as radio-iodination precursors is demonstrated through the labelling of [ 125 I]IMTO (iodometomidate) and [ 125 I]MIBG (meta-iodobenzylguanidine) thus offering an alternative to radio-iododestannylation processes using non-toxic precursors.
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