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α,ω-双-[对-氨基苯氧基]-烷类化合物对感染日本血吸虫病实驗动物有作用,但毒性較高,经改变其結构,将氨基移至苯核內侧,对位用甲基,卤素或硝基替代,成N,N′-双-(对-取代苯基)-α,ω-烷二胺类化合物,以察其化学結构和疗效的关系。 N,N′-双-(对-取代苯基)-α,ω-烷二胺类化合物由对-甲苯磺酰对-取代苯胺,氫氧化鈉和α,ω-二溴烷类在乙醇中縮合成N,N′-双-(对-甲苯磺酰)-N,N′-双-(对-取代苯基)-α,ω-烷二胺,然后用氫溴酸和苯酚进行水解而得,其中溴代化合物水解时核上溴原子可能脫落,所以用盐酸水解之。此类化合物中N,N′-双-(对-氯苯基)-α,ω-庚二胺和N,N′-双-(对-溴苯基)-α,ω-庚二胺另由相应的对-取代苯胺和-α,ω-二溴烷类及碳酸氫鈉在乙醇中縮合制备。
α, ω-bis- [p-aminophenoxy] -alkanes play an important role in the experimental animals infected with schistosomiasis japonica, but their toxicity is high. By changing their structure, the amino groups are transferred to the inside of benzene nucleus, Methyl, halogen or nitro, into N, N’-bis- (p-substituted phenyl) -α, ω-alkanediamine compounds to check the relationship between the chemical structure and efficacy. The N, N’-bis- (p-substituted phenyl) -α, ω-alkanediamines are prepared from p-toluenesulfonyl p-toluensilve, sodium hydroxide and α, ω-dibromoalkanes in ethanol (P-toluenesulfonyl) -N, N’-bis- (p-substituted phenyl) -α, ω-alkanediamine, followed by hydrolysis with hydrobromic acid and phenol to give Derived bromine compounds which bromine atoms may fall off when hydrolyzed, so hydrolysis with hydrochloric acid. N, N’-bis- (p-chlorophenyl) -α, ω-heptanediamine and N, N’-bis- (p-bromophenyl) -α, ω-heptanediamine in this class of compounds It is prepared by the condensation of the corresponding p-substituted aniline with -α, ω-dibromoalkanes and sodium bicarbonate in ethanol.