吲哚嗪衍生物的多组分一锅法合成  

Multi-component one-pot synthesis of indolizine derivatives

作　　者：陈丽 熊雨婷 郝天辉 周博 贾慧婷 严胜骄[1] CHEN Li;XIONG Yuting;HAO Tianhui;ZHOU Bo;JIA Huiting;YAN Shengjiao(School of Chemical Science and Technology,Yunnan University,Kunming 650500,Yunnan,China)

机构地区：[1]云南大学化学科学与工程学院,云南昆明650500

出　　处：《云南大学学报（自然科学版）》2024年第4期743-750,共8页Journal of Yunnan University(Natural Sciences Edition)

基　　金：国家级大学生创新创业训练项目(202210673071);云南省高校科技创新团队(C17624011121).

摘　　要：以吡啶乙酸乙酯1和苄溴类化合物2为原料,以原甲酸三乙酯为添加剂、Cs_(2)CO_(3)做碱,以乙腈为溶剂,回流反应7 h,四组分“一锅法”合成了多取代吲哚嗪衍生物3a~3i.实验中发现原甲酸三乙酯在反应体系中作为干燥剂能极好地除去反应体系中残余的微量水分,保证反应顺利进行.所合成的产物都经^(1)H NMR、^(13)C NMR和HRMS表征.结果表明,该方法具有原料易得,操作简单,路线简洁等特点,为筛选具有潜在生物活性的吲哚嗪衍生物提供了新的合成方法.In this paper,polysubstituted indolizine derivative 3 was synthesized with ethyl pyridine acetate 1 and benzyl bromide 2 as raw materials,triethyl orthoformate as additive and Cs_(2)CO_(3) as base in acetonitrile solution by reflux reaction for 7 h.The yield was medium to excellent.It was also found that triethyl orthoformate had water absorption in the reaction system.The synthesized products were characterized by ^(1)H NMR,^(13)C NMR and HRMS.The method described in the paper highlights the advantages of easily accessible raw materials,simple reaction procedure,and a straightforward synthesis route.This method offers a new approach for the synthesis of potential bioactive indolizine derivatives,which could be useful in the discovery of new drug candidates or bioactive compounds.

关 键 词：苄溴 吡啶乙酸乙酯 吲哚嗪 原甲酸三乙酯 多组分 

分 类 号：O621.3[理学—有机化学]