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本文制备了3α-溴-表苦鬼臼脂素,首次在鬼臼脂素结构修饰中在C环3-位引入取代基.其体外抑制KB细胞和L1210白血病细胞活性均高于阳性对照药.在碱性条件下,其可被方便地转化为4β-羟基-2,3-不饱和苦鬼臼脂素,进而2,3-不饱和鬼臼脂素衍生物可被合成.由于具有较好的体外抑制肿瘤细胞活性,该化合物可作为结构修饰的先导化合物.由于3-位溴原子的引入,其又是鬼臼脂素类化合物结构转化的中间体.“,”3α-bromo-epipicropodophyllin was prepared and its inhibition activities against KB cells and L1210 leukemia cells in vitro are higher than those of VP-16, a widely used drug in clinic at present. This is the f1rst time to introduce substitution at C-3 of ring-C in the work of modifying structure of podophyllotoxin. It can be transformed easily to 4β-hydroxy-2,3-ene-apopicropodophyllin under basic condition, so that, corresponding derivatives of 2,3-ene-apopicropodophyllin with substitution on carbon-4 could be synthesized. This compound can be regarded not only as a leading compound to be modified because of its antitumor activities, but also as an intermediate for the structure transformation.