CU(I) Supported Isotopic Exchange of Arylbound Iodide: New Future for Fast High Yield Labelling

The labelling methods for the radioiodination of aryl-compounds, based on nucleophilic isotopic exchange, which have been described until now, can be summarized as follows: Cu(II) catalysed reactions (1–6) (NH4)2SO4 solid state transfer methods (6–8) and reactions occurring in liquid phase (pseudo melt) in absence of any catalyst (6,9,10).

These methods were shown to give low and/or poorly reproducible labelling yields with the generation of labelled by-products and/or radioiodine. This implies that time consuming and costly purifications are required when the patient friendly but expensive short-lived I123 is involved.