2-氨基苯甲醇及其衍生物是一类很重要的具有双官能团的化合物,在有机化学和药物合成中具有广泛的用途.本文主要提供了一种简单、有效合成2-(芳氨基乙基氨基)苯甲醇类化合物的方法,同时测定了目标化合物的杀菌活性.溴乙酰芳胺与2-氨基苯甲醇经N-烷基化反应生成2-[(2-羟甲基苯基)氨基]乙酰芳胺类化合物3,然后经LiAlH4还原生成了一系列结构新颖的2-(芳氨基乙基氨基)苯甲醇类化合物5a ～ 5i,产率为76％ ～95％.用IR、1H NMR、13C NMR和元素分析等对产物结构进行了表征.目标化合物的杀菌活性结果表明,在测试浓度下,大部分显示中等至良好的活性,化合物5e对辣椒疫霉病菌的抑制活性达73.0％.
2-Aminobenzyl alcohol and its derivatives are a kind of important bifunctional compounds,and has found wide application in organic chemistry and drug synthesis.An efficient and simple method for synthesis of 2-(arylaminoethylamino) benzyl alcohols was described and the fungicidal activities of the target compounds were evaluated in this paper.N-alkylation of 2-aminobenzyl alcohol with bromoacetyl aryl amines produced 2-[(2-hydroxymethylphenyl)amino] acetyl aryl amines 3a ～3i,which were reduced by LiAlH4 giving a series of novel 2-(arylaminoethylamino) benzyl alcohols 5a ～ 5i in 76％ ～ 95％ yields.All the structures of the target compounds were characterized by the infrared spectroscopy (IR),proton nuclear magnetic resonance spectroscopy (1H NMR),13C NMR and elemental analysis.Most of compounds show moderate to good fungicidal activities under the testing concentration.Compound 5e shows 73％ activity of against Phytophythora capsici.
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