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Published on: October 10, 2016
Base-Mediated Radio-Iodination of Arenes by Using Organosilane and Organogermane as Radiolabelling Precursors
Hugo Bloux1, Amit Dahiya2, Alexandra Hébert1
1Centre d'Etudes et de Recherche sur le Médicament de Normandie (CERMN), Normandie Univ, UNICAEN, 14000, Caen, France.
Abstract:
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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