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Cu(I)-catalyzed one-pot reactions of isatins,indoles, and amines toward unsymmetrically substituted 2-carbonylarylureas
Authors:Xiangjun Peng  Xianyun Xu  Shuangyang Chen  Zeng Tian  Liangxian Liu  Qian Liu
Affiliation:1. Key Laboratory of Organo-Pharmaceutical Chemistry of Jiangxi Province, Gannan Normal University, Ganzhou 341000, PR China;2. School of Pharmaceutical Science, Gannan Medical University, Ganzhou 341000, PR China;3. Department of Pediatric Surgery, The First Affiliated Hospital of Gannan Medical University, Ganzhou 341000, PR China;4. Experimental Teaching Centre of Medical Morphology, Basic Medical Sciences School of Gannan Medical University, Ganzhou 341000, PR China
Abstract:A series of unsymmetrical arylureas was obtained by the one-pot method for reacting isatins with indoles incorporating primary amino moieties, a significant heterocyclic skeleton for diverse pharmaceutically active structures. The reaction proceeds through Cu(I)-catalyzed C2/>C3 bond of the ring-opening isatins and then expands the substrates in the optimum conditions. Furthermore, selected compounds <strong>4b</strong> and <strong>4k</strong> exhibit moderate to good anti-schistosomicidal activities.</td>
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Keywords:Unsymmetrical arylurea  Isatin  One-pot synthesis  Antischistosomicidal activity
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