二芳基肟苄醚类化合物的合成及杀菌活性  

Synthesis and Fungicidal Activities of Biaryl Methanone O-Benzyl Oximes

作　　者：李秀云[1] 万川[1] 杜士杰[1] 李红[1] 袁会珠[2] 蒋家珍[1] 肖玉梅[1] 覃兆海[1] 

机构地区：[1]中国农业大学理学院,北京100193 [2]中国农业科学院植物保护研究所,北京100193

出　　处：《高等学校化学学报》2015年第12期2415-2420,共6页Chemical Journal of Chinese Universities

基　　金：国家"十二五"科技支撑计划项目(批准号:2015BAK45B01)资助~~

摘　　要：以吡啶芳酮为原料,合成了11个含二芳基肟醚结构单元的甲氧丙烯酸酯类化合物,通过氢核磁共振谱(~1H NMR)、碳核磁共振谱(^(13)C NMR)和高分辨质谱(HRMS)等方法对其结构进行了确证.离体杀菌活性测定结果表明,该类化合物对供试的7种植物病原菌普遍表现出较高的抑制活性,其中化合物5d和5g的活性与对照药剂嘧菌酯和肟菌酯相当.进一步活体盆栽验证实验结果表明,在400 mg/L浓度下,部分化合物表现出很好的防治效果,如化合物5h对小麦白粉病和黄瓜炭疽病的防治效果达100%.另外,该类化合物对稻梨孢的孢子萌发具有强烈的抑制作用,在25 mg/L浓度下,绝大多数化合物的抑制率达到100%,但对灰葡萄孢的孢子萌发普遍无效.研究结果显示该类化合物具有进一步开发的价值.To discover new strobilurin analogs with high pesticidal activity, 11 novel methoxy acrylates bearing biaryl methanone oxime ether moieties were synthesized from aroyl pyridines, and characterized by ^1H and ^13C NMR and HRMS. In vitro fungicidal evaluation indicated that all of the target compounds exhibi- ted excellent activities against tested seven phytopathogenic fungi, and compounds 5d and 5g displayed compa- rable overall activities to azoxystrobin and trifloxystrobin. Some of the target compounds also exhibited excellent in vivo control effects at 400 rag/L, for example, compound 5h could 100% control wheat powdery mildew and cucumber anthracnose. Furthermore, at 25 mg/L, these compounds, including control agents, completely inhibited spores germination of rice blast, but no effect at all for cucumber gray mold. These results suggested that this class of compounds might deserve to be developed as new potential agricultural fungicides.

关 键 词：甲氧丙烯酸酯 吡啶苯基肟 苄基醚 杀菌活性 

分 类 号：O625.43[理学—有机化学]