Application of Microreactor to the Preparation of C-11-Labeled Compounds via O-[C-11]Methylation with [C-11]CH3I: Rapid Synthesis of [C-11]Raclopride

作者：Kawashima Hidekazu; Kimura Hiroyuki; Nakaya Yuta; Tomatsu Kenji; Arimitsu Kenji; Nakanishi Hiroaki; Ozeki Eiichi; Kuge Yuji; Saji Hideo^*

来源：Chemical & Pharmaceutical Bulletin, 2015, 63(9): 737-740.

• microreactor
• [C-11]raclopride
• O-[C-11]methylation
• [C-11]CH3I
• positron emission tomography

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.

• 出版日期2015-9