Multistep synthesis of a radiolabeled imaging probe using integrated microfluidics
Multistep synthesis of a radiolabeled imaging probe using integrated microfluidics
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DOI：
10.1126/science.1118919
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发表时间：
2005-12-16
期刊：
影响因子：
56.9
通讯作者：
Tseng, HR
中科院分区：
文献类型：
--
作者：
Lee, CC;Sui, GD;Tseng, HR
微反应器技术已显示出优化合成效率的潜力，特别是在制备敏感化合物方面。我们在集成微流控装置中合成了[F-18]氟标记的分子成像探针2-脱氧-2-[F-18]氟-D-葡萄糖（[F-18]FDG）。五个连续的过程-[F-18]氟化物浓度，水蒸发，放射性同位素，溶剂交换，水解脱保护-进行高放射化学产率和纯度，并与较短的合成时间相对于传统的自动化合成。制备用于小鼠正电子发射断层扫描成像研究的多剂量[F-18] FDG。这些结果，这构成了一个自动化的多步合成的原则在纳克至微克规模的证明，可以推广到一系列的放射性标记的基板。
Microreactor technology has shown potential for optimizing synthetic efficiency, particularly in preparing sensitive compounds. We achieved the synthesis of an [F-18]fluoride-radiolabeled molecular imaging probe, 2-deoxy-2-[F-18]fluoro-D-glucose ([F-18]FDG), in an integrated microfluidic device. Five sequential processes-[F-18]fluoride concentration, water evaporation, radiofluorination, solvent exchange, and hydrolytic deprotection-proceeded with high radiochemical yield and purity and with shorter synthesis time relative to conventional automated synthesis. Multiple doses of [F-18[FDG for positron emission tomography imaging studies in mice were prepared. These results, which constitute a proof of principle for automated multistep syntheses at the nanogram to microgram scale, could be generalized to a range of radiolabeled substrates.