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Synthesis of 1‐Aryl‐1H‐indazoles via a Ligand‐Free Copper‐ Catalyzed Intramolecular Amination Reaction
Authors:Mingshan Gao  Xiujie Liu  Xianyang Wang  Qian Cai  Ke Ding
Institution:1. Key Laboratory of Regenerative Biology and Institue of Chemical Biology, Guangzhou Institutes of Biomedicine and Health, Chinese Academy of Sciences, Guangzhou, Guangdong 510530, China;2. Jiangsu Provincial Institute of Materia Medica, Nanjing University of Technology, Nanjing, Jiangsu 210009, China
Abstract:A general synthesis of 1‐aryl‐1‐H‐indazoles from o‐halogenated aryl aldehydes or ketones and aryl hydrazines was described. This protocol included an intermolecular condensation and a ligand‐free copper‐catalyzed intramolecular Ullmann‐type coupling reaction. This method was applied to a wide range of substrates to produce the indazole products in good yields.
Keywords:copper  amination  ligand free
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