One-Pot Synthesis of Benzodiazepines through RuII-Catalyzed Regioselective [5+2] Annulation of N-Aryl Amidines with Alkynyl Cyclobutyl Acetates期刊界 All Journals 搜尽天下杂志传播学术成果专业期刊搜索期刊信息化学术搜索

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One-Pot Synthesis of Benzodiazepines through RuII-Catalyzed Regioselective [5+2] Annulation of N-Aryl Amidines with Alkynyl Cyclobutyl Acetates

Authors:	Jian Shen Bo Cui Junwei Huang Prof Dr Shenghui Lin Prof Dr Xiuling Cui

Institution:	1. Engineering Research Centre of Molecular Medicine of Ministry of Education, Key Laboratory of Fujian Molecular Medicine, Key Laboratory of Precision Medicine and Molecular Diagnosis of Fujian Universities, Key Laboratory of Xiamen Marine and Gene Drugs, School of Biomedical Sciences, Huaqiao University, Xiamen, 361021 P. R. China School of Biomedical Sciences, Huaqiao University, Quanzhou, 362021 P. R. China;2. School of Biomedical Sciences, Huaqiao University, Quanzhou, 362021 P. R. China;3. Engineering Research Centre of Molecular Medicine of Ministry of Education, Key Laboratory of Fujian Molecular Medicine, Key Laboratory of Precision Medicine and Molecular Diagnosis of Fujian Universities, Key Laboratory of Xiamen Marine and Gene Drugs, School of Biomedical Sciences, Huaqiao University, Xiamen, 361021 P. R. China

Abstract:	A highly efficient strategy to construct benzod]1,3]diazepines via selective C−H bond activation of N-aryl amidines and coupling with alkynyl cyclobutyl acetates was achieved successfully by Ru^II-catalyzed 5+2] cyclization. This protocol features excellent regioselectivity, wide substrate tolerance, mild reaction conditions, which might be potentially applied in the discovery of lead compounds for the developing new drugs.

Keywords:	[5+2] Cyclization Alkynyl cyclobutyl acetates Benzodiazepines N-Aryl amidines Ruthenium catalysis

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