Chin. J. Org. Chem. ›› 2014, Vol. 34 ›› Issue (11): 2296-2303.DOI: 10.6023/cjoc201404043 Previous Articles     Next Articles



李成坤a, 姜林a, 王悦a, 万福贤a, 张沛之a, 李映a, 崔紫宁b   

  1. a 山东农业大学化学与材料科学学院 泰安 271018;
    b 华南农业大学资源环境学院 广州 510642
  • 收稿日期:2014-04-24 修回日期:2014-05-20 发布日期:2014-07-02
  • 通讯作者: 李映,;崔紫宁,;
  • 基金资助:


Design, Synthesis and Biological Activities of N-(Substitutedbenzoyl)-N'-(5-methoxyl-2-methylsulfanylpyrimidin-4-amino)(thio) Ureas

Li Chengkuna, Jiang Lina, Wang Yuea, Wan Fuxiana, Zhang Peizhia, Li Yinga, Cui Ziningb   

  1. a College of Chemistry and Material Science, Shandong Agricultural University, Taian 271018;
    b South China Agricultural University, Guangzhou 510642
  • Received:2014-04-24 Revised:2014-05-20 Published:2014-07-02
  • Supported by:

    Project supported by the Promotive Research Fund for Excellent Young and Middle-aged Scientists of Shandong Province (No.BS2011NY013), the Innovation Fund for the Youth of Shandong Agricultural University (No.23682), the National Natural Science Foundation of China (No.21102173), the Project of Development of Science and Technology of Shandong Province (No.2013GZX20109) and the President Science Foundation of South China Agricultural University (No.4200-K13014).

In order to find new lead compounds with high effciency, low toxicity and environmental-friendly contribution, a series of novel N-(substituted benzoyl)-N'-(5-methoxyl-2-methylsulfanylpyrimidin-4-amino)(thio) ureas were designed and synthesized from substituted benzoic acids, α-methoxyl methyl acetate and ethyl formate. Their structures were confirmed by 1H NMR, IR and elemental analysis. The preliminary bioassay results indicated that some compounds exhibited considerate fungicidal activity. Among them compounds 10m and 10p showed more than 70% inhibitory rate to Botrytis cinerea and Sclerotinia sclerotiorum at 50 mg/mL, and the inhibitory rate against Sclerotinia sclerotiorum was higher than the control fungicide 95% chlorothalonil. Some compounds showed obvious insect growth regulation activity against 2~3 instar Culex larvae, compounds 10o and 10r showed 97.8% revised uneclosion rate, and compound 10t exhibited 100% insecticidal activity.

Key words: benzoylurea, pyrimidine, chitin, fungicidal activity, insect growth regulation activity