外式双环[2.2.1]庚烷(庚-5-烯)-2,3-二甲酸酐膦二肽衍生物的合成

选择有机磷基团对斑蝥素的结构骨架进行修饰改造,以外式双环2.2.1]庚-5-烯-2,3-二甲酸酐为原料,设计合成了一系列斑蝥素类似物。化合物的结构经1HNMR,MS及元素分析确证。

Studies on Synthesis of Phosphonodipeptide Derivatives of exo-Bicyclo[2.2.1]heptane(or hept-5-ene)-2,3-dicarboxylic Anhydride

Cantharidin, the active constituent of Mylabris, has displayed significant antitumor activities in vitro and in vivo. The adverse effects on urinary and gastrointestinal tracts prevent it from being accepted by the clinic. In order to search for new antitumor drugs with a high activity and low toxicity, a series of phosphonodipeptide derivatives of exo-bicyclo2.2.1]heptane (or hept-5-ene )-2, 3-dicarboxylic anhydride were synthesized by the condensation of the corresponding amino acid derivatives of exo-bicyclo2. 2. 1] hept-5-ene-2, 3-dicarboxylic anhydride with a-aminoalkylphosphonate, and their structures were confrimed by 1H NMR, MS and elemental analysis.