Convenient and efficient access to tri-and tetra-substituted 4-fluoropyridines via a[3+2]/[2+1]cyclization reaction

查看全文 作　　者：Xuejiao [1]Tang;Kun [1]Liu;Zeming [1]Qu;Junyan [1]Zhan;Rukui [1]Zhu;Fan [3]Teng;Lili [1]Meng;Yanmin [1]Huang;Chusheng [1]Huang;Yimiao [1]He;Qiang [1,2]Zhu

机构地区：[1]Guangxi Key Laboratory of Natural Polymer Chemistry and Physics,College of Chemistry and Materials,Nanning Normal University,Nanning 530001,China;[2]Guangzhou Institutes of Biomedicine and Health,Chinese Academy of Sciences,Guangzhou 510530,China;[3]Key Laboratory of Jiangxi Province for Persistent Pollutants Control and Resources Recycle,Nanchang Hangkong University,Nanchang 330063,China

出　　处：《Chinese Chemical Letters》索引2022年第33卷第6期,共5页

基　　金：the National Natural Science Foundation of China(Nos.21861007,21702034);Natural Science Foundation of Guangxi Province(No.2021GXNSFAA075024);“BAGUI Scholar”Program of Guangxi Province of China;High-Level Innovation Team and Distinguished Scholar Program in Guangxi Colleges and Universities;the Jiangxi Province Science and Technology Project(No.20212BAB213024)。 摘　　要：A[3+2]/[2+1]cycloaddition reaction of gem–difluorocyclopropenes is presented,offering a mild and efficient approach to accessing tri-and tetra-substituted 4-fluoropyridines in moderate to good yields with excellent regioselectivity.Multiple synthetic applications,including process-scale reactions,modification of bioactive molecules,derivatization reactions and synthesis of the analogue of the PKM2 modulator,are subsequently described. 关键词：4-Fluoropyridine gem-Difluorocyclopropene [3+2]/[2+1]cyclization reaction DMSO as an oxidant Regioselectivity PKM2 modulator

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Convenient and efficient access to tri-and tetra-substituted 4-fluoropyridines via a[3+2]/[2+1]cyclization reaction

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