3-吡啶甲酰基吲哚类化合物的合成研究  

Synthesis of 3-Picolinoylindole Derivatives

作　　者：徐孟华 沈梦婷 王盈盈 黄乐浩 XU Meng-hua;SHEN Meng-ting;WANG Ying-ying;HUANG Le-hao(School of Pharmaceutical Sciences,Wenzhou Medical University,Wenzhou 325035,China;Renji College,Wenzhou Medical University,Wenzhou 325035,China)

机构地区：[1]温州医科大学药学院,浙江温州325035 [2]温州医科大学仁济学院,浙江温州325035

出　　处：《化学试剂》2020年第11期1381-1384,共4页Chemical Reagents

基　　金：浙江省自然科学基金项目(LY18B020010);温州医科大学校级课题项目(wyx2018101105)。

摘　　要：为了发展一种高效简便合成标题化合物的方法,使用N-烷基芳香胺和吡啶甲酰基烯胺作为反应底物,通过考察催化剂、氧化剂、反应温度及溶剂对反应的影响来获得最优的反应条件。在最优反应条件下,吡啶甲酰基烯胺的sp^2 C—H键与N-烷基芳香胺的邻位sp2 C—H键通过交叉氧化脱氢环化反应,一步即高区域选择性地合成了7个标题化合物。产物均通过1HNMR、13CNMR和HR-MS等分析方法进行结构表征。We employ N-alkylanilines and picolinoylenamines as the substrates to develop an efficient and convenient method for the synthesis of the title compounds.The optimal reaction was obtained by investigating the influence of catalyst,oxidant,reaction temperature and solvent on the reaction.In the optimized reaction conditions,the seven high-value title compounds were synthesized via oxidative cross-coupling of the sp2 C—H bonds of picolinoylenamines with sp^2 C—H bonds of N-alkylanilines.The structures of all compounds were confirmed by 1HNMR,13CNMR and HR-MS.

关 键 词：钯催化 氧化偶联反应 N-烷基芳香胺 吡啶甲酰基烯胺 3-吡啶甲酰基吲哚 

分 类 号：O626.13[理学—有机化学]