钯催化吲哚-3-酮与芳基卤化物的直接C(sp)-H芳基化反应：一种合成亲核性2-单芳基化吲哚-3-酮的新颖高效方法。
Palladium-catalyzed direct C(sp)-H arylation of indole-3-ones with aryl halides: a novel and efficient method for the synthesis of nucleophilic 2-monoarylated indole-3-ones.
作者信息
Zhao Yong-Long, Tang Yong-Qin, Fei Xing-Hai, Xiao Tao, Lu Ya-Dong, Fu Xiao-Zhong, He Bin, Zhou Meng, Li Chun, Xu Peng-Fei, Yang Yuan-Yong
机构信息
State Key Laboratory of Functions and Applications of Medicinal Plants, School of Pharmacy, Engineering Research Center for the Development and Application of Ethnic Medicine and TCM (Ministry of Education), Guizhou Medical University Guiyang 550004 P. R. China
State Key Laboratory of Applied Organic Chemistry, College of Chemistry & Chemical Engineering, Lanzhou University Lanzhou 730000 P. R. China
出版信息
RSC Adv. 2018 Jul 16;8(45):25292-25297. doi: 10.1039/c8ra04807j.
A novel and efficient method for the synthesis of nucleophilic 2-monoarylated indole-3-ones palladium-catalyzed direct C(sp)-H arylation of indole-3-ones with aryl halides has been developed. Various 2-monoarylated indole-3-ones were readily obtained with yields up to 95%. As a class of important nucleophilic intermediates, 2-monoarylated indole-3-ones can be used for the construction of C2-quaternary indolin-3-one skeletons.
已开发出一种新颖且高效的合成亲核性2-单芳基化吲哚-3-酮的方法——钯催化吲哚-3-酮与芳基卤化物的直接C(sp)-H芳基化反应。各种2-单芳基化吲哚-3-酮均可轻松制得，产率高达95%。作为一类重要的亲核中间体，2-单芳基化吲哚-3-酮可用于构建C2-季碳吲哚啉-3-酮骨架。
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