卢孝慈, 瞿德浩, 张其楷. α,ω-双-对-氨基苯氧基-戊烷及-庚烷-N,N′-双取代衍生物的合成J. 药学学报, 1958, 6(1): 39-44.
引用本文: 卢孝慈, 瞿德浩, 张其楷. α,ω-双-对-氨基苯氧基-戊烷及-庚烷-N,N′-双取代衍生物的合成J. 药学学报, 1958, 6(1): 39-44.
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LU SHIAO-TZE CH TE-HAO CHANG CHI-CHIEK, . SYNTHESIS OF N,N′-DISUBSTITUTED DERIVATIVES OF α,ω-BIS-(p-AMINOPHENOXY)-PENTANE AND HEPTANEJ. Acta Pharmaceutica Sinica, 1958, 6(1): 39-44.
Citation: LU SHIAO-TZE CH TE-HAO CHANG CHI-CHIEK, . SYNTHESIS OF N,N′-DISUBSTITUTED DERIVATIVES OF α,ω-BIS-(p-AMINOPHENOXY)-PENTANE AND HEPTANEJ. Acta Pharmaceutica Sinica, 1958, 6(1): 39-44.
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α,ω-双-对-氨基苯氧基-戊烷及-庚烷-N,N′-双取代衍生物的合成

SYNTHESIS OF N,N′-DISUBSTITUTED DERIVATIVES OF α,ω-BIS-(p-AMINOPHENOXY)-PENTANE AND HEPTANE

    摘要
  • 摘要: α,ω-双-对-氨基苯氧基-烷类化合物对感染日本血吸虫病的实驗动物具有显著的疗效,惟毒性較高,我們合成了α,ω-双-对-氨基苯氧基-戊烷及-庚烷的N,N′-双取代衍生物10种,希望疗效增加而毒性减低。n=5或7; R=H,R′=CH2SO3Na R=H,R′=CH2CN R=H,R′=COOC2H5 R,R′=-(CH2)5- R,R′=-(CH2)2O(CH2)2- 由相应的α,ω-双-对-氨基苯氧基-烷类和羟甲磺酸鈉作用生成α,ω-双-对-氨基苯氧基-戊烷(及-庚烷)-N,N′-双甲磺酸鈉。它和氰化鉀反应,即得相应的N,N′-双乙臍衍生物。α,ω-双-对-氨基苯氧基-戊烷(及-庚烷)-N,N′-双甲酸乙酯則由相应的α,ω-双-对-氨基苯氧基-烷类和氯代甲酸乙酯作用而得。α,ω-双-对-六氫呲啶基苯氧基-戊烷(及-庚烷)和α,ω-双-对-N-氧氮六圜基苯氧基-戊烷(及-庚烷)則分别由相当的α,ω-双-对-氨基苯氧基-烷类和二溴戊烷或β,β′-二溴乙醚作用生成。其中α,ω-双-对-N-六氫吡啶基苯氧基-戊烷井另由N-对羟苯基六氫吡啶和二溴戊烷縮合生成。

     

    Abstract: A series of α, ω-bis-(p-aminophenoxy)-alkanes was found to show high Schistosomicidal activity against experimental animals but having relatively high toxic effect.Therefore, we prepared ten compounds of N, N'-disubstituted derivatives of α, ω-bis-(paminophenoxy)-pentane and-heptane for the purpose of finding the most active and least toxic compound. n=5 or 7; R=H, R'=CH2SO3Na R=H, R'= CH2CN R=H, R'=COO2H3 R,R'=-(CH2)3-

     

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