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N-(取代苯氧乙酰基)-3-氨基-二氢噻吩-2-酮衍生物的合成和生物活性
Synthesis and bioactivity of N-(substituted phenoxyacetyl)-3-amino-dihydrothiophene-2-one derivatives
【摘要】 酰胺类化合物具有很高的药用活性,为了进一步研究酰胺衍生物的合成与性质,文中用3-氨基-二氢噻吩-2-酮盐酸盐与取代苯氧乙酸反应,得到N-(取代苯氧乙酰基)-3-氨基-二氢噻吩-2-酮衍生物。产物结构经IR、1H NMR和元素确证。对5种病原菌的抑菌活性进行了生物活性测试。合成中采用三氯氧磷为缩合试剂,采用一锅反应,简便易行,缩合试剂价廉易得、反应收率高,产物纯度较高,为此类新化合物的合成和筛选提供了依据。
【Abstract】 The amide compounds have high pharmaceutical activity.To further study the synthesis and properties of the amide compounds,N-(substituted phenoxyacetyl)-3-amino-dihydrothiophene-2-one derivatives were synthesized by the reaction of substituted phenoxyacetic acid with 3-amino-dihydrothiophene-2-one hydrochloride.The structures were confirmed by IR,1HNMR and elemental analysis.The antifungal activity of 5 pathogens were tested.Phosphorus oxychloride was used as the condensation reagent in synthesis.The method has advantages with one-pot synthesis,simple and easy operation,cheap and easily-obtained raw material,high yield and high purity.The results provide the basis for synthetizing and screening new compounds.
【Key words】 3-amino-dihydrothiophene-2-one; amide; benzoic acid; thienone; synthesis; bioactivity;
- 【文献出处】 化学工程 ,Chemical Engineering(China) , 编辑部邮箱 ,2013年05期
- 【分类号】TQ251.2
- 【下载频次】88