A simplified and improved synthesis of [11C]phosgene with iron and iron (III) oxide

Nuclear Medicine and Biology
Ken-ichi NishijimaN Tamaki

Abstract

[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.

Citations

Nov 28, 2012·Journal of Nuclear Cardiology : Official Publication of the American Society of Nuclear Cardiology·James T Thackeray, Frank M Bengel
Sep 22, 2010·Advanced Drug Delivery Reviews·Zibo Li, Peter S Conti
Sep 2, 2006·Yakugaku zasshi : Journal of the Pharmaceutical Society of Japan·Ken-ichi Nishijima
Nov 7, 2008·Angewandte Chemie·Philip W MillerAntony D Gee
May 16, 2013·Chemical Communications : Chem Comm·Benjamin H RotsteinNeil Vasdev
Mar 23, 2017·Current Cardiology Reports·Nabil E Boutagy, Albert J Sinusas
Jun 18, 2020·Nuclear Medicine and Biology·Toshimitsu FukumuraMing-Rong Zhang
Mar 10, 2020·Nuclear Medicine and Biology·Jonas ErikssonOleksiy Itsenko

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