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

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。

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.