@article{oai:repo.qst.go.jp:00046335, author = {Asakawa, Chiharu and Ogawa, Masanao and Fujinaga, Masayuki and Kumata, Katsushi and Xie, Lin and Yamasaki, Tomoteru and Yui, Joji and Fukumura, Toshimitsu and Zhang, Ming-Rong and 浅川 千春 and 小川 政直 and 藤永 雅之 and 熊田 勝志 and 謝 琳 and 山崎 友照 and 由井 譲二 and 福村 利光 and 張 明栄}, issue = {11}, journal = {Bioorganic & Medicinal Chemistry Letters}, month = {Apr}, note = {N-(2-{3-[3,5-Bis(trifluoromethyl)]phenylureido}ethyl)glycyrrhetinamide (2), an ureido-substituted derivative of glycyrrhetinic acid (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 2 using [11C]phosgene ([11C]COCl2) as a labeling agent with the expectation that [11C]2 could become a positron emission tomography ligand for the imaging of proteasome and kinase in tumors. The strategy for the radiosynthesis of [11C]2 was to react hydrochloride of 3,5-bis(trifluoromethyl)aniline (4HCl) with [11C]COCl2 to possibly give isocyanate [11C]6, followed by the reaction of [11C]6 with N-(2-aminoethyl) glycyrrhetinamide (3).}, pages = {3594--3597}, title = {Utilization of [11C]phosgene for radiosynthesis of N-(2-{3-[3,5-bis(trifluoromethyl)] phenyl[11C]ure2;ido}ethyl)glycyrrhetinamide, an inhibitory agent for proteasome and kinase in tumors}, volume = {22}, year = {2012} }