Continuous-Flow Synthesis of N-Succinimidyl 4-[18F]fluorobenzoate Using a Single Microfluidic Chip.
Continuous-Flow Synthesis of N-Succinimidyl 4-[18F]fluorobenzoate Using a Single Microfluidic Chip.
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DOI：
10.1371/journal.pone.0159303
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发表时间：
2016
期刊：
影响因子：
3.7
通讯作者：
Saji H
中科院分区：
文献类型：
--
作者：
Kimura H;Tomatsu K;Saiki H;Arimitsu K;Ono M;Kawashima H;Iwata R;Nakanishi H;Ozeki E;Kuge Y;Saji H
在正电子发射断层扫描(PET)放射化学领域，紧凑型微反应堆提供了可靠和可重复的合成方法，减少了用于放射性标记的昂贵前体的使用，并有效地利用了热室中有限的空间。为了开发更紧凑的微反应器来辐射合成多步过程所需的18F标记化合物，我们尝试了通过使用微反应器的三步过程来辐射合成N-琥珀酰亚胺4-[18F]氟苯甲酸酯([18F]SFB)。我们使用间歇反应器和微反应器研究了[18F]SFB的各个步骤，并开发了一种新的具有单个微流控芯片的连续流动合成方法，以实现快速高效的[18F]SFB的放射合成。用这种连续流动法合成[18F]SFB，在6.5min内成功地完成了三步反应，放化产率为±2%(n=5)。此外，在[18F]SFB标记牛血清白蛋白的实验中，用该方法合成的[18F]SFB与常规方法合成的[18F]SFB的质量相当。
In the field of positron emission tomography (PET) radiochemistry, compact microreactors provide reliable and reproducible synthesis methods that reduce the use of expensive precursors for radiolabeling and make effective use of the limited space in a hot cell. To develop more compact microreactors for radiosynthesis of 18F-labeled compounds required for the multistep procedure, we attempted radiosynthesis of N-succinimidyl 4-[18F]fluorobenzoate ([18F]SFB) via a three-step procedure using a microreactor. We examined individual steps for [18F]SFB using a batch reactor and microreactor and developed a new continuous-flow synthetic method with a single microfluidic chip to achieve rapid and efficient radiosynthesis of [18F]SFB. In the synthesis of [18F]SFB using this continuous-flow method, the three-step reaction was successfully completed within 6.5 min and the radiochemical yield was 64 ± 2% (n = 5). In addition, it was shown that the quality of [18F]SFB synthesized on this method was equal to that synthesized by conventional methods using a batch reactor in the radiolabeling of bovine serum albumin with [18F]SFB.