Fully Substituted Pyrazoles Assisted Palladium-Catalyzed Late-Stage Arylation of C-H Bond

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作者: Fu, Xiaopan Wang, Yangyang Yang, Jinyue Wu, Gaorong Xia, Chengcai Ji, Yafei

作者单位: Engineering Research Centre of Pharmaceutical Process Chemistry, Ministry of Education, School of Pharmacy, East China University of Science & Pharmacy College, Shandong First Medical University & Technology, Shanghai, 200237, China Shandong Academy of Medical Sciences, Tai'an, 271016, China

摘要: A successful protocol has been developed for palladium-catalyzed late-stage arylation of fully substituted pyrazoles. Through screening of optimazation of reaction parameters, the most efficient reaction conditions for mono-ortho-position arylation were obtained. This reaction features a broad substrate scope, good functional group tolerance as well as good to excellent yield. Moreover, the intermolecular competition experiments and gram scale reaction were also performed. The kinetic isotopic e...更多; A successful protocol has been developed for palladium-catalyzed late-stage arylation of fully substituted pyrazoles. Through screening of optimazation of reaction parameters, the most efficient reaction conditions for mono-ortho-position arylation were obtained. This reaction features a broad substrate scope, good functional group tolerance as well as good to excellent yield. Moreover, the intermolecular competition experiments and gram scale reaction were also performed. The kinetic isotopic effect result reveled C-H bond cleavage was involved in the rate-limiting step and a plausible mechanism was proposed based on the dual-core dimeric palladacycle.收起

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