Synthesis, Structure Characterization and Fungicidal Activity of 1,3-Disubstituted-1H-1,2,4-triazole-5-amines

文献类型: 外文期刊

第一作者: Jia Changqing

作者: Jia Changqing;Xu Yanjun;Liu Jiping;Qin Zhaohai;Su Wangcang

作者机构:

关键词: 1H-1,2,4-triazole-5-amine;synthesis;intramolecular cyclization;fungicidal activity

期刊名称:CHINESE JOURNAL OF ORGANIC CHEMISTRY ( 影响因子:1.652; 五年影响因子:1.2 )

ISSN: 0253-2786

年卷期: 2016 年 36 卷 4 期

页码:

收录情况: SCI

摘要: A novel series of 1,3-disubstituted-1H-1,2,4-triazole-5-amines were synthesized via hydrazinolysis, condensation, alkylation and acid-catalyzed intramolecular cyclization starting from nitroguanidine 1. Their structures were characterized by IR, H-1 NMR, C-13 NMR and HRMS analysis. The preliminary bioassay indicated that most of them showed certain extent of growth inhibition in vitro against six phytopathogen fungi. Compared with other target compounds, 1-(n-butyl)-3-(4-chlorophenyl)-1H-1,2,4-triazole-5-amine (6y) was found to have high activity and the widest fungicidal spectrum. Its inhibition rates to five pathogens were all above 53%. This kind of compounds could be synthesized and derived easily, and were valuable as lead structure for future developing novel fungicides.

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