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

尹艳清 YYQ


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.


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