Radiosynthesis of SPECT tracers via a copper mediated 123I iodination of (hetero)aryl boron reagents

Abstract

A general method for the copper mediated nucleophilic ¹²³I-iodination of (hetero)aryl boronic esters and acids has been developed. The broad substrate scope of this radiosynthetic approach allows access to [¹²³I]DPA-713, [¹²³I]IMPY, [¹²³I]MIBG and [¹²³I]IPEB that are four commonly used SPECT radiotracers. Our results infer that aryl boronic reagents can now be employed as common precursors for both fluorine-18 and iodine-123 radiolabelling.