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含5-氟脲嘧啶齐聚物的合成

SYNTHESIS OF OLIGOMERS CONTAINING 5-FLUOROURACIL

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【作者】 朴爱植孙树门

【Author】 Piao Aichih and Sun Shumen (Institute of Chemistry, Academia Sinica)

【机构】 中国科学院化学研究所中国科学院化学研究所

【摘要】 <正> 5-氟脲嘧啶是用于治疗肺癌、肾癌、乳癌、结肠癌等癌变的药物。虽然5-氟脲嘧啶具有上述疗效,但在临床应用时,尚存在恶心,呕吐,腹泻,白细胞、血小板下降等副作用。更为严重的缺点,是既对肿瘤细胞有活性,同时也作用于正常细胞,为克服此缺点,将抗癌药物与低分子化合物结合,诸如激素、磺胺,这些是已知能集聚在一定组织内药物,但利用此法,迄今也很少获得成效。

【Abstract】 The condensation oligomers of 5-fluorouracil were prepared by reacting 2, 4 bis-(trimethylsilylxy)5-fluoropyrimidine with various dicarboxylic chlorides, e.g.The structural characteristics of the oligomers obtained were investigated by IR, 1HNMR. The oligomers were then hydroly zed in acid, alkaline and neutral medium at room temperature respectively and the amount of 5-fluorouracil released was guan-titated by measuring its absorbance at 266.5 nm. However, in the case of oligomers containing phenyleme moiety, 5-fluorouracil was not detected, when the hydrolysis was conducted in acid or neutral medium, while in the case of oligomers containing methy-lene moiety, hydrolysis proceeded readily in acid, alkaline and neutral medium.

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