Hevesy Laboratory, Center for Nuclear Technologies, Technical University of Denmark, Risø Campus, Frederiksborgvej 399, P.O. Box 49, 4000 Roskilde, Denmark.
Molecules. 2013 Aug 30;18(9):10531-47. doi: 10.3390/molecules180910531.
The polymer supported phosphazene bases PS-P₂(tBu) and the novel PS-P₂(PEG) allowed for efficient extraction of [¹⁸F]F⁻ from proton irradiated [¹⁸O]H₂O and subsequent radiofluorination of a broad range of substrates directly on the resin. The highest radiochemical yields were obtained with aliphatic sulfonates (69%) and bromides (42%); the total radiosynthesis time was 35-45 min. The multivariate analysis showed that the radiochemical yields and purities were controlled by the resin load, reaction temperature, and column packing effects. The resins could be reused several times with the same or different substrates. The fully automated on-column radiofluorination methodology was applied to the radiosynthesis of the important PET radiotracers [¹⁸F]FLT and [¹⁸F]FDG. The latter was produced with 40% yield on a 120 GBq scale and passed GMP-regulated quality control required for commercial production of [1¹⁸F]FDG. The combination of compact form factor, simplicity of [¹⁸F]F⁻ recovery and processing, and column reusability can make solid phase radiofluorination an attractive radiochemistry platform for the emerging dose-on-demand instruments for bedside production of PET radiotracers.
聚合物负载的磷杂环戊二烯碱基 PS-P₂(tBu) 和新型 PS-P₂(PEG) 可从质子辐照的 [¹⁸O]H₂O 中有效提取 [¹⁸F]F⁻，并可直接在树脂上对广泛的底物进行放射性氟化。最高的放射化学产率是用脂肪族磺酸盐（69%）和溴化物（42%）获得的；总放射合成时间为 35-45 分钟。多元分析表明，放射化学产率和纯度受树脂负载、反应温度和柱填充效应的控制。这些树脂可以在相同或不同的底物上重复使用几次。全自动柱上放射性氟化方法学已应用于重要的 PET 放射性示踪剂 [¹⁸F]FLT 和 [¹⁸F]FDG 的放射合成。后者以 40%的产率在 120GBq 规模上生产，并通过了 GMP 监管的质量控制，这是 [1¹⁸F]FDG 商业生产所必需的。紧凑的外形、[¹⁸F]F⁻回收和处理的简单性以及柱的可重复使用性，使得固相放射性氟化成为新兴的按需剂量仪器床边生产 PET 放射性示踪剂的有吸引力的放射化学平台。
