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1.对乙酰氨基苯酚与1,7-二溴代庚烷,在乙醇钠液中缩合,得1,7-双(对乙酰氨基苯氧基)-庚烷,经稀盐酸水解制得1,7-双(对氨基苯氧基)-庚烷二盐酸盐.2.对乙酰氨基硫酚在硷醇中分别与1,3-二溴代丙烷,1,6-二溴代己烷和1,7-二溴代庚烷缩合,水解就可以分别得到相应的α,ω-双(对氨基苯硫基)-烷二盐酸盐.3.1-氯代甘油及1,3-二溴代甘油与对乙酰氨基苯酚或硫酚缩合,再行水解后,分别获得甘油的1-(对氨基苯基)及1,3-双(对氨基苯基)-醚或其硫代醚.4.1,6-二氯代-2,3-4,5-二亚甲基-D-甘露醇与对乙酰氨基苯酚钠盐,在封闭管中长期加热,可获得2,3-4,5-二亚甲基-D-甘露醇-1,6-双(对乙酰氨基苯)-醚.5.将 D-甘露醇做成1,2-3,4-5,6-三异丙基-D-甘露醇,经部分水解成3,4-异丙基化合物,再制成1,6-双(对甲苯磺酰基)-2,5-二乙酰基-3,4-异丙基-D-甘露醇,在乙醇钠溶液中,分别与对乙酰氨基苯酚或硫酚缩合,再经水解,即分别得到 D-甘露醇-1,6-双(对氨基苯基)-醚或 D-甘露醇-1,6-双(对氨基苯基)硫代醚的双盐酸盐.6.对硝基苯酚与1,4-二溴代-2-丁烯缩合,生成1,4-双(对硝基苯氧基)-2-丁烯,于双键上进行双羟基化,并将硝基还原,得1,4-双(对氨基苯氧基)-2,3-threo-双羟基丁烷二盐酸盐.7.本文报导中的11个化合物,其中除Ⅰ、Ⅴ外,均为未知化合物,用作动物试验,初步结果表明,这些多羟基的氨苯氧(或硫)烷类化合物,对日本住血吸虫病都无效.
1. Acetaminophen and 1,7-dibromoheptane in sodium acetate solution condensation to give 1,7-bis (p-acetamidophenoxy) -heptane, diluted hydrochloric acid obtained 1, 7-Bis (p-aminophenoxy) -heptane dihydrochloride. 2. Acetaminothiol is reacted with 1,3-dibromopropane, 1,6-dibromohexane and The corresponding α, ω-bis (p-aminophenylthio) -alkane dihydrochloride can be obtained by the condensation of 1, 7-dibromoheptane and hydrolysis respectively.1.1-Chloroglycerol and 1,3-dibromo Glycerol is condensed with paracetamol or thiophenol and further hydrolyzed to give 1- (p-aminophenyl) and 1,3-bis (p-aminophenyl) -ethers of glycerol or their thioethers, respectively. 4.1, Dichloro-2,3,4,5-dimethylene-D-mannitol and sodium acetaminophen, long-term heating in a closed tube to obtain 2,3-4,5-sub-sub Methyl-D-mannitol-1,6-bis (p-acetamidophenyl) ether 5. D-mannitol was prepared as 1,2-3,4-5,6-triisopropyl-D- Mannitol, partially hydrolyzed to 3,4-isopropyl compound, and then made into 1,6-bis (p-toluenesulfonyl) -2,5-diacetyl-3,4-isopropyl-D- Alcohol, sodium ethoxide solution, respectively, with acetaminophen or thiophene condensation, and then by water Solution to give the dihydrochloride of D-mannitol-1,6-bis (p-aminophenyl) -ether or D-mannitol-1,6-bis (p- aminophenyl) thioether, respectively. The condensation of p-nitrophenol with 1,4-dibromo-2-butene gives 1,4-bis (p-nitrophenoxy) -2-butene, which is double hydroxylated on the double bond and The nitro group is reduced to give 1,4-bis (p-aminophenoxy) -2,3-threo-hydroxybutyrate dihydrochloride.7. The 11 compounds reported herein, except for compounds I and V , All of which are unknown compounds, are used as animal experiments. The preliminary results show that these polyhydroxy-phenylalanine (or sulfur) alkanes are ineffective against living schistosomiasis in Japan.