Chinese Journal of Organic Chemistry ›› 2020, Vol. 40 ›› Issue (2): 528-535.DOI: 10.6023/cjoc201907034 Previous Articles     Next Articles


丁成荣, 潘亚运, 谭成侠   

  1. 浙江工业大学化学工程学院 杭州 310032
  • 收稿日期:2019-07-24 修回日期:2019-09-08 发布日期:2019-10-12
  • 通讯作者: 谭成侠
  • 基金资助:

Synthesis and Biological Activity of Aryl Thiazole Piperidine Amide Compounds

Ding Chengrong, Pan Yayun, Tan Chengxia   

  1. College of Chemical Engineering Science, Zhejiang University of Technology, Hangzhou 310032
  • Received:2019-07-24 Revised:2019-09-08 Published:2019-10-12
  • Supported by:
    Project supported by the Collaborative Innovation Center of Zhejiang Province Green Pesticide.

In order to find a novel biologically active compound containing aromatic thiazole piperidine structure, 15 novel aryl thiazole piperidine amide derivatives were designed and synthesized. The structures of the target compounds were fully characterized by 1H NMR, 13C NMR and HRMS spectra. The bioactivity test showed that some target compounds had good fungicidal and insecticidal activity. For example, the inhibition rate of 5-(3-bromophenyl)-4-methyl-2-(1-((4-nitrophenyl)-sulfonyl)piperidin-4-yl)thiazole (6b) against Pseudoperonospora cubensis was 100% better than azoxystrobin, and the inhibition rate of 5-(4-bromophenyl)-2-(1-((4-chlorophenyl)sulfonyl)piperidin-4-yl)-4-methylthiazole (6c) against Rhizoctonia solani was 58.86% comparable to azoxystrobin at 200 μg/mL. The lethal rate of (4-(5-(3-bromophenyl)-4-methylthiazol-2-yl) piperidin-1-yl) (m-tolyl)methanone (6h) against Mythimna separata was 100% at 500 μg/mL.

Key words: piperidinylthiazole, aromatic structure, fungicidal activity, insecticidal activity