A Fluorine-18 Radiolabeling Method Enabled by Rhenium(I) Complexation Circumvents the Requirement of Anhydrous Conditions

Mitchell A Klenner; Giancarlo Pascali; Bo Zhang; Tiffany R Sia; Lawson K Spare; Anwen M Krause-Heuer; Janice R Aldrich-Wright; Ivan Greguric; Adam J Guastella; Massimiliano Massi; Benjamin H Fraser

doi:10.1002/chem.201700440

A Fluorine-18 Radiolabeling Method Enabled by Rhenium(I) Complexation Circumvents the Requirement of Anhydrous Conditions

Chemistry. 2017 May 11;23(27):6499-6503. doi: 10.1002/chem.201700440. Epub 2017 Apr 11.

Authors

Mitchell A Klenner^{1

2}, Giancarlo Pascali^{1

3}, Bo Zhang^{1

4}, Tiffany R Sia^{1

3}, Lawson K Spare⁵, Anwen M Krause-Heuer¹, Janice R Aldrich-Wright⁵, Ivan Greguric¹, Adam J Guastella³, Massimiliano Massi², Benjamin H Fraser¹

Affiliations

¹ Australian Nuclear Science and Technology Organisation (ANSTO), New Illawarra Rd, Lucas Heights, New South Wales, Australia.
² Department of Chemistry, Curtin University, Kent St, Bentley, Western Australia, Australia.
³ Brain and Mind Centre, The University of Sydney, Mallett St, Camperdown, New South Wales, Australia.
⁴ Monash University, Wellington Road, Clayton, Victoria, Australia.
⁵ School of Science and Health, Western Sydney University, Penrith, New South Wales, Australia.

PMID: 28332244
DOI: 10.1002/chem.201700440

Abstract

Azeotropic distillation is typically required to achieve fluorine-18 radiolabeling during the production of positron emission tomography (PET) imaging agents. However, this time-consuming process also limits fluorine-18 incorporation, due to radioactive decay of the isotope and its adsorption to the drying vessel. In addressing these limitations, the fluorine-18 radiolabeling of one model rhenium(I) complex is reported here, which is significantly improved under conditions that do not require azeotropic drying. This work could open a route towards the investigation of a simplified metal-mediated late-stage radiofluorination method, which would expand upon the accessibility of new PET and PET-optical probes.

Keywords: fluorine-18 radiolabeling; late-stage fluorination; microfluidics; pet chemistry; rhenium complexes.