Radiosynthesis of SPECT tracers via a copper mediated 123I iodination of (hetero)aryl boron reagents. Issue 90 (24th October 2016)

• Record Type: Journal Article
• Authors: Wilson, Thomas C.; McSweeney, Greg; Preshlock, Sean; Verhoog, Stefan; Tredwell, Matthew; Cailly, Thomas; Gouverneur, Véronique
• Is Part Of: Chemical communications. Volume 52:Issue 90(2016)
• Page Start: 13277
• Page End: 13280
• Publication Date: 2016-10-24
• Subjects: Chemistry -- Periodicals; 540
• DOI: 10.1039/c6cc07417k
• Languages: English
• ISSNs: 1359-7345

Abstract

Abstract : The Cu-mediated [ 123 I]iodination of aryl boronic pinacol esters and acids exhibits broad scope and is successfully applied to the labelling of four radiotracers, [ 123 I]DPA-713, [ 123 I]IMPY, [ 123 I]MIBG and [ 123 I]IPEB. Abstract : A general method for the copper mediated nucleophilic 123 I-iodination of (hetero)aryl boronic esters and acids has been developed. The broad substrate scope of this radiosynthetic approach allows access to [ 123 I]DPA-713, [ 123 I]IMPY, [ 123 I]MIBG and [ 123 I]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.