有机化学 ›› 2019, Vol. 39 ›› Issue (3): 867-872.DOI: 10.6023/cjoc201806029 上一篇    下一篇

研究简报

N-烷氧基取代酰胺类化合物的合成及杀菌活性

黄朋勉a, 周智慧a, 杜永磊b, 庞怀林b, 吕亮b   

  1. a 长沙理工大学化学与食品工程学院 长沙 410114;
    b 上海泰禾国际贸易有限公司 上海 200335
  • 收稿日期:2018-06-19 修回日期:2018-09-05 发布日期:2018-10-26
  • 通讯作者: 黄朋勉, 吕亮 E-mail:huangpengmian@126.com;liang_lv@cacch.com
  • 基金资助:

    长沙市科技计划(Nos.kq1801163,kq1801052)和湖南省水生资源食品加工工程技术研究中心开放基金(No.2018KJY08)资助项目.

Synthesis and Fungicidal Activity of N-Alkoxyl Amide Derivatives

Huang Pengmiana, Zhou Zhihuia, Du Yongleib, Pang Huailinb, Lü Liangb   

  1. a School of Chemistry and Food Engineering, Changsha University of Science and Technology, Changsha 410114;
    b CAC Shanghai International Trading Co., Ltd., Shanghai 200335
  • Received:2018-06-19 Revised:2018-09-05 Published:2018-10-26
  • Contact: 10.6023/cjoc201806029 E-mail:huangpengmian@126.com;liang_lv@cacch.com
  • Supported by:

    Project supported by the Changsha Science and Technology Project (Nos. kq1801163, kq1801052) and the Hunan Provincial Engineering Research Center for Food Processing of Aquatic Biotic Resources (No. 2018KJY08).

为寻找具有高杀菌活性的农药先导化合物,采用活性亚结构拼接的方法,将吡唑醚菌酯结构中羟基吡唑结构片段引入氟唑菌酰羟胺的结构中,合成了12个结构新颖的N-烷氧基酰胺类化合物.目标化合物的结构经过1H NMR,13C NMR和HRMS确证.杀菌活性测试表明,在测试浓度下,一些目标化合物对亚洲大豆锈病、黄瓜霜霉病或黄瓜白粉病表现出了一定的防效,其中化合物3a在100 mg/L测试浓度下对黄瓜白粉病的防效为95%.

关键词: 氟唑菌酰羟胺, 酰胺, 农药, 杀菌活性

In order to find lead compounds with high fungicidal activity, the phenyl moiety of pydiflumetofen was replaced by substituted 1-phenyl-3-hydroxylpyrazole moiety of pyraclostrobin according to the method of active substructure combination. 12 novel N-alkoxyl amides were synthesized and their structures were confirmed by 1H NMR, 13C NMR and HRMS. Preliminary fungicidal activity screening results showed that some analogues exhibited certain fungicidal activity against Phakopsora pachyrhizi, Pseudoperonospora cubensis or Erysiphe cichoracearum, compound 3a displayed 95% protective effect against Erysiphe cichoracearum at 100 mg/L.

Key words: pydiflumetofen, amide, pesticide, fungicidal activity