Nishijima Ken-ichi, Kuge Yuji, Seki Koh-ichi, Ohkura Kazue, Motoki Noriko, Nagatsu Kotaro, Tanaka Akira, Tsukamoto Eriko, Tamaki Nagara
Department of Tracer Kinetics, Graduate School of Medicine, Hokkaido University, Kita 15 Nishi 7, Kita-ku, 060-8638, Sapporo, Japan.
Nucl Med Biol. 2002 Apr;29(3):345-50. doi: 10.1016/s0969-8051(01)00310-9.
[11C]Phosgene ([11C]COCl2), a useful precursor for labeling several radiopharmaceuticals, is generally produced by catalytic oxidation of [11C]carbon tetrachloride over Fe granules, although in low yields or with poor reproducibility. In order to develop am improved synthesis of [11C]phosgene, two oxidizing agents, Fe2O3 and CuO, were examined. The yield of [11C]phosgene was significantly increased using Fe2O3 powder mixed with Fe granules, while the use of CuO alone, or CuO powder mixed with Fe granules resulted in an insignificant yield. The yield and specific activity of S- (-) [11C]CGP-12177 synthesized using Fe2O3 powder mixed with Fe granules were markedly higher than those synthesized by the previous methods using Fe granules alone or Fe granules mixed with Fe powder. Thus, in the present study, we developed a simple and practical method for the synthesis of [11C]phosgene, which provided an improved yield of S- (-) [11C]CGP-12177.
[11C]光气（[11C]COCl2）是标记多种放射性药物的有用前体，通常通过[11C]四氯化碳在铁颗粒上的催化氧化来制备，但其产率较低或重现性较差。为了开发一种改进的[11C]光气合成方法，研究了两种氧化剂，即Fe2O3和CuO。使用与铁颗粒混合的Fe2O3粉末时，[11C]光气的产率显著提高，而单独使用CuO或与铁颗粒混合的CuO粉末产率不显著。使用与铁颗粒混合的Fe2O3粉末合成的S-(-)[11C]CGP-12177的产率和比活度明显高于以前单独使用铁颗粒或铁颗粒与铁粉混合的方法合成的结果。因此，在本研究中，我们开发了一种简单实用的[11C]光气合成方法，该方法提高了S-(-)[11C]CGP-12177的产率。
