Application of Microreactor to the Preparation of C-11-Labeled Compounds via O-[11C]Methylation with [11C]CH3I: Rapid Synthesis of [11C]Raclopride
Application of Microreactor to the Preparation of C-11-Labeled Compounds via O-[11C]Methylation with [11C]CH3I: Rapid Synthesis of [11C]Raclopride
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DOI：
10.1248/cpb.c15-00365
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发表时间：
2015-09-01
影响因子：
1.7
通讯作者：
Saji, Hideo
中科院分区：
文献类型：
--
作者：
Kawashima, Hidekazu;Kimura, Hiroyuki;Saji, Hideo
建立了一种新的放射性标记方法，用于[C-11]雷氯必利的快速合成。设计了带有Y形混合接头的芯片，该Y形混合接头具有200 μ m（宽）× 20 μ m（深）× 250 mm（长）的流动通道，并评价了O-[C-11]甲基化的效率。通过注射器将含有O-去甲基前体或[C-11] CH 3 I的二甲基亚砜溶液引入单独的注射口，并在各种条件下测量放射化学产率。微反应器衍生的[C-11]雷氯必利的衰变校正放射化学产率在25 ℃下20秒内达到12%，观察到随温度升高而增加。相比之下，在25 ℃下的分批合成产生5%的产率：这表明该装置可以在更短的时间内有效地实现O-[C-11]甲基化。微反应器技术可以通过[C-11] CH 3 I与O-[C-11]甲基化促进简单有效的常规C-11标记化合物的生产。
A new radiolabeling method using a microreactor was developed for the rapid synthesis of [C-11]raclopride. A chip bearing a Y-shaped mixing junction with a 200 mu m (width)X20 mu m (depth)x250 mm (length) flow channel was designed, and the efficiency of O-[C-11]methylation was evaluated. Dimethyl sulfoxide solutions containing the O-desmethyl precursor or [C-11]CH3I were introduced into separate injection ports by infusion syringes, and the radiochemical yields were measured under various conditions. The decay-corrected radiochemical yield of microreactor-derived [C-11]raclopride reached 12% in 20s at 25 degrees C, which was observed to increase with increasing temperature. In contrast, batch synthesis at 25 degrees C produced a yield of 5%: this indicates that this device could effectively achieve O-[C-11]methylation in a shorter period of time. The microreactor technique may facilitate simple and efficient routine production of C-11-labeled compounds via O-[C-11]methylation with [C-11]CH3I.