Article ID Journal Published Year Pages File Type
1374041 Bioorganic & Medicinal Chemistry Letters 2012 4 Pages PDF
Abstract

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 (4·HCl) with [11C]COCl2 to possibly give isocyanate [11C]6, followed by the reaction of [11C]6 with N-(2-aminoethyl)glycyrrhetinamide (3).

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Physical Sciences and Engineering Chemistry Organic Chemistry
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