Use of SF6 for the production of electrophilic 18F-fluorination reagents
: Anna Krzyczmonik, Thomas Keller, Anna K. Kirjavainen, Salla Lahdenpohja, Sarita Forsback, Olof Solin
Publisher: Elsevier B.V.
: 2017
: Journal of Fluorine Chemistry
: Journal of Fluorine Chemistry
: 204
: 90
: 97
: 8
: 0022-1139
: 1873-3328
DOI: https://doi.org/10.1016/j.jfluchem.2017.10.010
Electrophilic 18F-fluorination is an important method for production of tracers for positron emission tomography. The most commonly employed 18F-fluorination reagents [18F]F2, [18F]Selectfluor bis(triflate) and [18F]NFSi
allow for the synthetically simple and fast introduction of fluorine-18
into organic molecules, in particular those containing electron rich
aromatic rings. For the time being the best method for the production of
[18F]F2 gas, the most common electrophilic
reagent, is a post-target production which applies a high voltage
electrical discharge to promote the 19F/18F isotopic exchange between [18F]MeF and carrier F2 gas. The aim of this study was to develop a new method for the production of electrophilic 18F-fluorination reagents which would avoid use of toxic and very reactive carrier F2 gas. In this study the use of SF6 as an alternative to carrier F2 gas was tested. Experiments were carried out in two different matrix gases: Ne and Xe. The electrophilic 18F-fluorination reagent produced was used for the labelling of two model compounds (6-[18F]fluoro-L-DOPA and [18F]Selectfluor bis(triflate)) in order to prove its feasibility. This proof-of-concept study showed that SF6 in Xe can be used in place of F2 for the production of electrophilic [18F]F2 gas. When SF6 in Ne was used only trace amounts of [18F]F2 was observed.