Rapid Aqueous Late-Stage Radiolabelling of [GaF3 (BnMe2 -tacn)] by 18 F/19 F Isotopic Exchange: Towards New PET Imaging Probes

Francesco M Monzittu; Imtiaz Khan; William Levason; Sajinder K Luthra; Graeme McRobbie; Gillian Reid

doi:10.1002/anie.201802446

Rapid Aqueous Late-Stage Radiolabelling of [GaF₃ (BnMe₂ -tacn)] by ¹⁸ F/¹⁹ F Isotopic Exchange: Towards New PET Imaging Probes

Angew Chem Int Ed Engl. 2018 May 28;57(22):6658-6661. doi: 10.1002/anie.201802446. Epub 2018 Apr 26.

Authors

Francesco M Monzittu¹, Imtiaz Khan², William Levason¹, Sajinder K Luthra², Graeme McRobbie², Gillian Reid¹

Affiliations

¹ School of Chemistry, University of Southampton, Southampton (UK), SO17 1BJ, UK.
² GE Healthcare, The Grove Centre, White Lion Road, Amersham (UK), HP7 9LL, UK.

Abstract

A simple and rapid method for ¹⁸ F radiolabelling of [GaF₃ (BnMe₂ -tacn)] by ¹⁸ F/¹⁹ F isotopic exchange is described. The use of MeCN/H₂ O or EtOH/H₂ O (75:25) and aqueous [¹⁸ F]F^- (up to 200 MBq) with heating (80 °C, 10 min) gave 66±4 % ¹⁸ F incorporation at a concentration of 268 nm, and 37±5 % ¹⁸ F incorporation at even lower concentration (27 nm), without the need for a Lewis acid promoter. A solid-phase extraction method was established to give [Ga¹⁸ F¹⁹ F₂ (BnMe₂ -tacn)] in 99 % radiochemical purity in an EtOH/H₂ O mixture.

Keywords: fluorine-18; gallium; isotopic exchange; positron emission tomography; radiofluorination.

Publication types

Research Support, Non-U.S. Gov't