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

Thomas L. Wilson (1) , Greg Mcsweeney (2) , Sean Preshlock (2) , Stefan Verhoog (2) , Matthew Tredwell (2) , Thomas Cailly (3) , Veronique Gouverneur (2)

1 ESO - European Southern Observatory
2 Chemistry Research Laboratory [Oxford, UK]
3 CERMN - Centre d'Etudes et de Recherche sur le Médicament de Normandie

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.

Domaines: Radiochimie

Thomas L. Wilson, Greg Mcsweeney, Sean Preshlock, Stefan Verhoog, Matthew Tredwell, et al.. Radiosynthesis of SPECT tracers via a copper mediated 123 I iodination of (hetero)aryl boron reagents. Chemical Communications, 2016, 52 (90), pp.13277-13280. ⟨10.1039/C6CC07417K⟩. ⟨hal-02011093⟩