钯催化的7-氮杂吲哚的3位芳基化反应  

Palladium-catalyzed C3-arylation of 7-azaindole

作　　者：刘珊珊 赵晨[1] 周鲜颖 马养民 LIU Shan-shan;ZHAO Chen;ZHOU Xian-ying;MA Yang-min(College of Chemistry and Chemical Engineering,Shaanxi University of Science&Technology,Xi′an 710021,China;Shaanxi Key Laboratory of Chemical Additives for Industry,Xi′an 710021,China)

机构地区：[1]陕西科技大学化学与化工学院,陕西西安710021 [2]陕西科技大学陕西省轻化工助剂重点实验室,陕西西安710021

出　　处：《陕西科技大学学报》2020年第5期91-95,102,共6页Journal of Shaanxi University of Science & Technology

基　　金：中国博士后科学基金面上项目(2018M643806XB);陕西省科技厅自然科学基金项目(2019JQ-787);陕西科技大学博士科研启动基金项目(2016BJ-23)。

摘　　要：7-氮杂吲哚是一类重要的杂环类化合物,具有特殊的理化和药理性质,在医药、农药、及食品等领域都有着广泛用途.以7-氮杂吲哚为底物,在钯催化下,通过与芳基硼酸反应合成多种C3位芳基取代的7-氮杂吲哚衍生物,探索了一条钯催化的7-氮杂吲哚C3选择性芳基化反应的路线,该方法从易得的N未保护的7-氮杂吲哚出发,合成路线简洁,产率中等至优.建立了7-氮杂吲哚化合物向下游重要生物活性分子转化的方法体系和理论基础.7-Azaindole is an important class of heterocyclic compounds with special physical and chemical properties and pharmacological properties.It is widely used in medicine,pesticides,and food.In this paper,7-azaindole was used as a substrate to react with an aryl boric acid,providing arylated product at the C3 position under palladium catalysis.Finally,we developed palladium-catalyzed C3 arylation of 7-azaindole from unprotected 7-azaindoles,which present a concise and effective way to construct 7-azaindole derivatives.The method is a basis for the conversion of 7-azaindole compounds to important biologically active molecules.

关 键 词：7-氮杂吲哚 钯催化 选择性 芳基化反应 

分 类 号：O626[理学—有机化学]