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以4-氰基苯酚和2-氯丙酸乙酯(或2-氯乙酸甲酯)为起始原料进行反应,得到2-(4-(1H-四唑-5-基)苯氧基)丙酸/乙酸酯,进而发生Huisgen反应合成了一系列新型1,3,4-噁二唑类标题化合物,其结构经~1H NMR,~(13)C NMR,IR,MS及元素分析或高分辨质谱得到表征和确认.用X射线衍射测定了化合物3q的晶体结构.初步生物活性测试结果表明,含有较小体积取代基的噁二唑化合物3c和3d在200μg/mL测试浓度下对水稻KARI酶分别具有94.5%和83.1%的抑制活性.化合物3p在100μg/mL浓度下对双子叶油菜(Brassica campestris)胚根生长抑制率可达82.4%.
The reaction was carried out using 4-cyanophenol and ethyl 2-chloropropionate (or methyl 2-chloroacetate) as starting materials to give 2- (4- (1H-tetrazol-5- yl) phenoxy) Propionic acid / acetic acid ester, then a series of new 1,3,4-oxadiazole compounds were synthesized by Huisgen reaction. The structures of the compounds were characterized by 1H NMR, 13C NMR, IR, MS and elemental analysis or The crystal structure of compound 3q was determined by X-ray diffraction.The preliminary bioassay results showed that the oxadiazole compounds 3c and 3d containing a smaller volume of substituent groups had higher activity against rice at the test concentration of 200μg / mL KARI enzyme had 94.5% and 83.1% inhibitory activities, respectively.Compound 3p inhibited the radicle growth of Brassica campestris to 82.4% at the concentration of 100μg / mL.