CuⅠ催化吡咯酰胺化反应合成吡咯-1-酰胺化合物  

CuⅠ-catalyzed Amidation of Pyrroles for the The Synthesis of Pyrrole-1-amides

作　　者：谭平[1] 晏山舒 吴红谕 陈锦杨 许新华[3] TAN Ping;YAN Shanshu;WU Hongyu;CHEN Jinyang;XU Xinhua(School of Mechanical Engineering, Hunan Mechanical and Electrical Polytechnic, Changsha 410151, China;College of Chemistry and Chemical Engineering, Yangtze Normal University, Fuling 408000, China;College of Chemistry and Chemical Engineering, Hunan University, Changsha 410082, China)

机构地区：[1]湖南机电职业技术学院机械工程学院,湖南长沙410151 [2]长江师范学院化学化工学院,重庆涪陵408000 [3]湖南大学化学化工学院,湖南长沙410082

出　　处：《合成化学》2022年第4期274-279,共6页Chinese Journal of Synthetic Chemistry

基　　金：国家自然科学基金资助项目(21273068)。

摘　　要：吡咯衍生物具有良好的生物活性,是很多药物和天然产物分子的重要组成部分。此外,吡咯衍生物在抗菌、抗结核、抗病毒、抗疟疾以及抗癌等方面的应用也非常广泛。本文报道了温和条件下,Cu(Ⅰ)催化吡咯与异氰酸酯N-甲酰胺化制备吡咯-1-酰胺化合物的反应,开发了一种简便的方法合成吡咯-1-酰胺化合物。该方法对多种异氰酸酯具有很好的适用性,均能以较高产率获得相应目标产物。与文献方法相比,本方法具有高效、操作简便、反应条件温和等优点。Pyrrole derivatives have good biological activity and are an important part of many drugs and natural product molecules. In addition, their application as antibacterial, anti-tuberculosis, antiviral,anti-malaria and anti-cancer agents was also studied. Here, we report a facile protocol for the synthesis of pyrrole-1-carboxamidesviathe copper(Ⅰ)-catalyzed N-carboxamidation of pyrrole with isocyanates under mild conditions. This process is scalable and tolerates a wide spectrum of isocyanates to deliver corresponding products in good to excellent yields. Comparing to the previous methods, this strategy has the advantages of high efficiency, simple operation, and mild conditions, providing an efficient approach to pyrrole-1-carboxamides.

关 键 词：CuⅠ催化 N-酰胺化反应 吡咯-1-酰胺化合物 吡咯 异氰酸酯 合成 

分 类 号：O626[理学—有机化学]