Utilization of [¹¹C]phosgene for radiosynthesis of N-(2-{3-[3,5-bis(trifluoromethyl)]phenyl[¹¹C]ureido}ethyl)glycyrrhetinamide, an inhibitory agent for proteasome and kinase in tumors

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• 作者：Chiharu Asakawa^a ; Masanao Ogawa^a ; ^b ; Masayuki Fujinaga^a ; Katsushi Kumata^a ; Lin Xie^a ; Tomoteru Yamasaki^a ; Joji Yui^a ; Toshimitsu Fukumura^a ; Ming-Rong Zhang^a ; ^{zhang@nirs.go.jp}
• 关键词：Proteasome ; Kinase ; [11C]urea ; [11C]phosgene ; PET
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2012
• 期刊代码：10_0960894x
• 类别：ch
• 出版时间：1 June, 2012
• 卷：22
• 期：11
• 页码：3594-3597
• 文件大小：336 K

摘要

<em>Nem>-(2-{3-[3,5-Bis(trifluoromethyl)]phenylureido}ethyl)glycyrrhetinamide (dFont">2), an ureido-substituted derivative of glycyrrhetinic acid (dFont">1), has been reported to display potent inhibitory activity for proteasome and kinase, which are overexpressed in tumors. In this study, we labeled this unsymmetrical urea dFont">2 using [¹¹C]phosgene ([¹¹C]COCl₂) as a labeling agent with the expectation that [¹¹C]dFont">2 could become a positron emission tomography ligand for the imaging of proteasome and kinase in tumors. The strategy for the radiosynthesis of [¹¹C]dFont">2 was to react hydrochloride of 3,5-bis(trifluoromethyl)aniline (dFont">4路HCl) with [¹¹C]COCl₂ to possibly give isocyanate [¹¹C]dFont">6, followed by the reaction of [¹¹C]dFont">6 with <em>Nem>-(2-aminoethyl)glycyrrhetinamide (dFont">3).