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タイトル: Application of Microreactor to the Preparation of C-11-Labeled Compounds via O-[11C]Methylation with [11C]CH3I: Rapid Synthesis of [11C]Raclopride.
著者: Kawashima, Hidekazu
Kimura, Hiroyuki
Nakaya, Yuta
Tomatsu, Kenji
Arimitsu, Kenji
Nakanishi, Hiroaki
Ozeki, Eiichi
Kuge, Yuji
Saji, Hideo
著者名の別形: 佐治, 英郎
キーワード: microreactor
[11C]raclopride
O-[11C]methylation
[11C]CH3I
positron emission tomography
発行日: 2015
出版者: Pharmaceutical Society of Japan
誌名: Chemical & pharmaceutical bulletin
巻: 63
号: 9
開始ページ: 737
終了ページ: 740
抄録: 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.
著作権等: © 2015 The Pharmaceutical Society of Japan
URI: http://hdl.handle.net/2433/207680
DOI(出版社版): 10.1248/cpb.c15-00365
PubMed ID: 26329868
出現コレクション:学術雑誌掲載論文等

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