Diels-Alder反应在斑蝥素衍生物合成中的应用  

Application of Diels-Alder reaction to the synthesis of cantharidin derivatives

作　　者：尹艳清[1] 黄超[1] 郭家辉[1] 李燕华[1] 杜银顺 杨丽娟[1] 

机构地区：[1]云南民族大学民族药资源化学国家民委-教育部重点实验室,云南昆明650500

出　　处：《云南民族大学学报（自然科学版）》2015年第2期115-118,共4页Journal of Yunnan Minzu University:Natural Sciences Edition

基　　金：国家自然科学基金(21202142);教育部重点项目(212161);民族药资源化学国家民族事务委员会-教育部重点实验室开放基金(MZY1115);云南民族大学2014年学生实验实践能力提升工程项目;云南民族大学化学与生物技术学院SRT科研项目(2013HXSRTZ01;2013HXSRTZ02;2013HXSRTZ06)

摘　　要：斑蝥素作为传统中药斑蝥的主要有效活性成分,在治疗肿瘤方面发挥重要作用.在对斑蝥素进行合成和改造过程中,Diels-Alder反应被广泛应用.以呋喃及其衍生物为双烯体,炔烃、马来酸酐为亲双烯体,两组分在回流或室温下就能发生成环反应获得斑蝥素基本骨架.以几类不同底物发生Diels-Alder反应制备斑蝥素衍生物并对实验条件进行了优化.As the main effective active ingredient of Blister Beetle,a traditional Chinese drug,cantharidin plays an important role in the treatment of malignant diseases. And Diels-Alder reaction is widely applied in the synthesis of its derivatives. With furan and its derivatives as the diene,alkyne or maleic anhydride as the dienophile,the basic framework of cantharidin can be generated by refluxing or under the room temperature. In this paper,the synthesis of cantharidin derivatives with different substrates by Diels-Alder reaction has been discussed and the experimental conditions have also been optimized.

关 键 词：DIELS-ALDER反应 斑蝥素 抗肿瘤 

分 类 号：R248.3[医药卫生—中医临床基础]