摘要/Abstract

为了从氰基丙烯酸酯类衍生物中寻找新的活性化合物，通过活性基团拼接方法，设计合成了一系列新型含噁唑环结构的氰基丙烯酸酯化合物.初步的除草活性测试结果表明，大部分标题化合物具有较好的除草活性.在剂量为750 g/ha时，部分化合物对芥菜的除草活性可达80%~100%，对小藜的抑制率可达90%~100%，对酸模的除草活性可达80%~100%.2-氰基-3-甲硫基-3-{[4-（2-（4-氟苯基）噁唑-4-基）甲硫基]-苯甲基胺基}丙烯酸（2-甲氧基）乙酯（11a）和2-氰基-3-甲硫基-3-{[4-（2-（3，4-二氟苯基）噁唑-4-基）甲硫基]-苯甲基胺基}丙烯酸（2-甲氧基）乙酯（11e）对看麦娘的除草活性分别为70%和60%，对棒头草的抑制率分别为70%和60%.化合物11a对早熟禾的抑制率为70%.此外，化合物11a在150 g/ha剂量下对芥菜和酸模的抑制率均达40%.
关键词: 氰基丙烯酸酯, 噁唑环, 合成, 生物活性
In order to find novel cyanoacrylate derivatives possessing potent bioactivities, a series of novel cyanoacrylates bearing substituted oxazole unit were designed and prepared. The bioassay data indicated that most title compounds had satisfactory herbicidal activities. At the dosage of 750 g/ha, some compounds showed herbicidal activity against Brassica juncea with 80%~100%, Chenopodium serotinum L. with 90%~100%, and Rumex acetosa L. with 80%~100%. 2-Cyano-3-me-thylthio-3-{[4-(2-(4-fluorophenyl)oxazole-4-yl)methylthio]-benzylanimo}acrylic acid (2-methoxy)ethyl ester (11a) and 2-cyano-3-methylthio-3-{[4-(2-(3,4-difluorophenyl)oxazole-4-yl)methylthio]-benzylanimo}acrylic acid (2-methoxy)ethyl ester (11e) displayed herbicidal activity against Alopecurus aequalis Sobol with 70% and 60%, and Polypogon fugax Nees ex Steud with 70% and 60%. Compound 11a showed herbicidal activity against Poa acroleuca Steud with 70%. In addition, the inhibitory rates of compound 11a against Brassica juncea and Rumex acetosa L. were both 40% at the dosage of 150 g/ha.
Key words: cyanoacrylate, oxazole unit, preparation, biological activity


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