1,3-偶极环加成构建3,5-二取代异噁唑类衍生物  

Construction of 3,5-Disubstituted Isoxazole Derivatives by 1,3-Dipolar Cycloaddition

作　　者：邓斌 程睿 黄洁 李子民 宁小珺 袁成 高涛 孙绍发 汪钢强 DENG Bin;CHENG Rui;HUANG Jie;LI Zimin;NING Xiaojun;YUAN Cheng;GAO Tao;SUN Shaofa;WANG Gangqiang(School of Pharmacy,Hubei University of Science and Technology,Xianning 437100,China;Hubei Key Laboratory of Radiation Chemistry and Functional Materials,School of Nuclear Technology and Chemistry & Biology,Hubei University of Science and Technology,Xianning 437100,China;School of Pharmaceutical Sciences,South-Central University for Nationalities,Wuhan 430074,China)

机构地区：[1]湖北科技学院药学院,湖北咸宁437100 [2]湖北科技学院核技术与化学生物学院辐射化学与功能材料湖北省重点实验室,湖北咸宁437100 [3]中南民族大学药学院,湖北武汉430074

出　　处：《化学与生物工程》2021年第6期12-18,39,共8页Chemistry & Bioengineering

基　　金：国家级科研项目培育计划项目(2019-21GP05);湖北省大学生创新创业项目(S202010927044)。

摘　　要：异噁唑是一类具有独特化学结构的杂环类化合物,具有广泛的生物活性和药物活性,在医药、农药以及有机合成等领域具有非常广阔的应用前景。研究了取代氯化肟与端位炔烃在碳酸铯作用下发生1,3-偶极环加成反应构建3,5-二取代异噁唑类衍生物的方法,通过1HNMR、13CNMR等对所得化合物结构进行了表征。该合成方法具有原料易得、操作简单、条件温和、普适性好、收率高、成本低等特点。Isoxazoles are a kind of heterocyclic compounds with unique chemical structures,which have a wide range of biological and pharmaceutical activities,and have a very broad application prospect in medicine,pesticides,and organic synthesis.In this paper,we studied the construction of 3,5-disubstituted isoxazole derivatives by 1,3-dipolar cycloaddition reaction between substituted chlorinated oxime and terminal alkynes under the action of cesium carbonate,and characterized their structures by 1HNMR and 13CNMR.The synthetic method has the advantages of easily-obtained raw materials,simple operation,mild conditions,good universality,high yield,and low cost.

关 键 词：3 5-二取代异噁唑类衍生物 异噁唑 1 3-偶极环加成 

分 类 号：O626[理学—有机化学]