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Use of SF6 for the production of electrophilic 18F-fluorination reagents
Journal of Fluorine Chemistry ( IF 1.9 ) Pub Date : 2017-10-31 , DOI: 10.1016/j.jfluchem.2017.10.010
Anna Krzyczmonik , Thomas Keller , Anna K. Kirjavainen , Salla Lahdenpohja , Sarita Forsback , Olof Solin

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.



中文翻译:

SF 6在生产亲电子18 F氟化试剂中的用途

亲电18 F氟化是生产正电子发射断层扫描示踪剂的重要方法。最常用的18 F氟化试剂[ 18 F] F 2,[ 18 F] Selectfluor双(三氟甲磺酸酯)和[ 18 F] NFSi可将氟18合成简单,快速地引入有机分子中,特别是那些含有丰富的电子芳香环。目前,作为生产[ 18 F] F 2气体(最常见的亲电试剂)的最佳方法,是一种目标后生产,它通过高压放电来促进19 F / 18[ 18 F] MeF与载气F 2气体之间的F同位素交换。

这项研究的目的是开发一种生产亲电18 F氟化试剂的新方法,该方法可避免使用有毒且反应性强的载体F 2气体。在这项研究中,测试了使用SF 6替代载气F 2气体的方法。实验是在两种不同的基质气体:Ne和Xe中进行的。为了证明其可行性,使用了亲电子的18 F氟化试剂标记了两种模型化合物(6- [ 18 F]氟-L -DOPA和[ 18 F] Selectfluor双(三氟甲磺酸酯))。

这项概念验证研究表明,Xe中的SF 6可以代替F 2用于生产亲电[ 18 F] F 2气体。当使用Ne中的SF 6时,仅观察到痕量的[ 18 F] F 2

更新日期:2017-10-31
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