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α,ω-双-[对-氨基苯氧基]-烷类对感染日本血吸虫病的实驗动物具有显著疗效,惟毒性较大.本文叙述了α,ω-双-[对-甲氨基苯氧基]-戊烷及-庚烷-N,N′双取代衍生物的合成,希望这些衍生物的毒性减低,而疗效增大.n=5或7.R=-CH_2SO·ONa,-CH_2SO_2·ONa,-CH_2COONa, -CH_2CONH_2,-CH_2CN,-CONH_2,-COCH_3,-CH_2CONH_2,-COOC_2H_5.N,N′-双甲亚磺酸鈉及N,N′-双甲磺酸鈉衍生物系以α,ω-双-[对-甲氨基苯氧基]-戊烷Ⅰ及庚烷Ⅱ分別与烴甲亚磺酸鈉及烴甲磺酸鈉在碱性甲醇中作用生成.N,N′-双甲磺酸鈉衍生物与氰化鉀反应得N,N′-双乙腈衍生物,再行水解則得N,N′-双乙酸鈉衍生物.由对-N-氨基碳酰甲基-N-甲氨基苯酚、对-N-氨基碳酰-N-甲氨基苯酚,以及对-N-β-羥乙基-N-甲氨基苯酚分別与α,ω-二溴烷类縮合,得N,N′-双乙酰胺、N,N′-双碳酰胺、以及N,N′-双-β-羥乙基衍生物.N,N′-双碳酰胺亦由Ⅰ及Ⅱ直接与氰酸鉀反应制得。N,N′-双甲酸乙酯衍生物系以Ⅱ与氯代甲酸乙酯作用合成,而N,N′-双乙酰衍生物則按常法制取之。
α, ω-bis- [p-aminophenoxy] -alkanes have significant curative effect on experimental animals infected with schistosomiasis japonica, but their toxicity is rather high.This paper describes the effects of α, ω-bis- [p- -pentane and -heptane-N, N ’-disubstituted derivatives, the toxicity of these derivatives is expected to decrease and the therapeutic effect is enhanced. N = 5 or 7. R = -CH 2 SO · ONa, -CH 2 SO 2 · ONa, -CH_2COONa, -CH_2CONH_2, -CH_2CN, -CONH_2, -COCH_3, -CH_2CONH_2, -COOC_2H_5.N, N’-bismethanesulfinate and sodium N, N’- , ω-bis- [p-methylaminophenoxy] -pentane Ⅰ and heptane Ⅱ are respectively reacted with sodium hydrocarbon methane sulfonate and sodium hydrocarbon methanesulfonate in basic methanol to form N, N’-bis Sodium methanesulfonate derivative reacted with potassium cyanide to obtain N, N’-diacetonitrile derivatives, and then hydrolyzed to obtain sodium N, N’-diacetate derivative. -methylaminophenol, p-N-aminocaproyl-N-methylaminophenol and p-N-β-hydroxyethyl-N-methylaminophenol respectively with α, ω-dibromoalkanes to yield N, N’-bisacetamide, N, N’-bis-carboxamide and N, N’-bis-β-hydroxyethyl derivatives N, N’-bis-carboxamide also from I and II directly with potassium cyanate You should be prepared. Ethyl N, N’-bis-carboxylate derivatives are synthesized by the reaction of II with ethyl chloroformate, while N, N’-diacetyl derivatives are prepared according to the usual method.