纪庆娥, 韦耀良. 心血管系统药物异黄酮化合物的合成J. 药学学报, 1989, 24(12): 906-912.
引用本文: 纪庆娥, 韦耀良. 心血管系统药物异黄酮化合物的合成J. 药学学报, 1989, 24(12): 906-912.
QE Ji, YL Wei. SYNTHESIS OF ISOFLAVONES AS CARDIOVASCULAR DRUGJ. Acta Pharmaceutica Sinica, 1989, 24(12): 906-912.
Citation: QE Ji, YL Wei. SYNTHESIS OF ISOFLAVONES AS CARDIOVASCULAR DRUGJ. Acta Pharmaceutica Sinica, 1989, 24(12): 906-912.

心血管系统药物异黄酮化合物的合成

SYNTHESIS OF ISOFLAVONES AS CARDIOVASCULAR DRUG

  • 摘要: 在黄豆甙元化学结构的基础上,合成了一系列异黄酮衍生物。由相应的脱氧安息香与N,N-二甲基甲酰胺缩二甲醇环合而得相应的异黄酮或与醋酐醋酸钠环合而为2-甲基异黄酮,再进行Mannich反应和醚化而得目的物。初筛表明化合物Ⅰ1~3,Ⅰ5,Ⅱ1,Ⅲ2有明显耐缺氧作用。Ⅰ1,Ⅰ5还有显著的扩张冠脉作用。

     

    Abstract: On the basis of the chemical structure of daidzein, a series of isoflavones have been synthesized. The intermediates, 7-methoxy-4'-hydroxyisoflavone(V) and 7-hydroxy-4'-methoxyisoflavone(Ⅸ) were prepared by condensation of corresponding desoxybenzoin with dimethylformamide dimethylacetal. 7-Methoxy-2-methyl-4'-hydroxyisoflavone (Ⅶ) was also prepared from desoxybenzoin Ⅳ by reacting with acetic anhydride and anhydrous sodium acetate and followed by hydrolysis.Compounds Ⅰ1~5 were obtained by Mannich reaction and compounds Ⅱ1,21,2 were obtained by etherification of corresponding isoflavones.All compounds were tested for resistance to hypoxia in mice and Ⅰ1~3, Ⅰ5, Ⅱ1 and Ⅲ2 were shown to have significant effect. Compound Ⅰ1 and Ⅰ5 were also found to increase coronary blood flow.

     

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