Kawashima Hidekazu, Kimura Hiroyuki, Nakaya Yuta, Tomatsu Kenji, Arimitsu Kenji, Nakanishi Hiroaki, Ozeki Eiichi, Kuge Yuji, Saji Hideo
Graduate School of Pharmaceutical Sciences, Kyoto University.
Chem Pharm Bull (Tokyo). 2015;63(9):737-40. doi: 10.1248/cpb.c15-00365.
A new radiolabeling method using a microreactor was developed for the rapid synthesis of [(11)C]raclopride. A chip bearing a Y-shaped mixing junction with a 200 µm (width)×20 µm (depth)×250 mm (length) flow channel was designed, and the efficiency of O-[11C]methylation was evaluated. Dimethyl sulfoxide solutions containing the O-desmethyl precursor or [11C]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 [11C]raclopride reached 12% in 20 s at 25 °C, which was observed to increase with increasing temperature. In contrast, batch synthesis at 25 °C produced a yield of 5%: this indicates that this device could effectively achieve O-[11C]methylation in a shorter period of time. The microreactor technique may facilitate simple and efficient routine production of 11C-labeled compounds via O-[11C]methylation with [11C]CH3I.
开发了一种使用微反应器的新放射性标记方法，用于快速合成[(11)C]雷氯必利。设计了一种带有Y形混合结的芯片，其流动通道宽度为200 µm、深度为20 µm、长度为250 mm，并评估了O-[11C]甲基化的效率。通过输液注射器将含有O-去甲基前体或[11C]CH3I的二甲亚砜溶液引入单独的注射端口，并在各种条件下测量放射化学产率。在25°C下，微反应器衍生的[11C]雷氯必利的衰变校正放射化学产率在20秒内达到12%，并且观察到随着温度升高而增加。相比之下，25°C下的批量合成产率为5%：这表明该装置可以在更短的时间内有效地实现O-[11C]甲基化。微反应器技术可能有助于通过用[11C]CH3I进行O-[11C]甲基化，简单而高效地常规生产11C标记的化合物。
