The palladium-mediated C–H radio-iodination of arenes using sodium iodide as the primary isotopic source is reported and performed without chemical know-how in 30 min and applied to the synthesis of complex radio-iodinated compounds of biological interest.

The radio-iodination of arenes is investigated from organosilane and organogermane precursors using ipsoelectrophilic halogenation (IEH). Discovery of a mild base mediated process allows radio-iodination in HFIP (1,1,1,3,3,3hexafluoro-2-propanol) of either aryl silane or germane, with germanes being more reactive. Clinical potential of arylger-manes 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.www.chemeurj.org

An improved protocol to perform C–H radio-iodination is described. These new conditions allow rapid and clean formation of radio-iodinated N-acylsulfonamides using [125I]NIS and catalytic amounts of palladium acetate and para-toluenesulfonic acid. No pre-functionalized precursors are required and the products are obtained with radiochemical conversions (RCC) of 27–84%.

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