文献类型： 外文期刊

作者： Jia Changqing ¹ ; Su Wangcang ² ; Xu Yanjun ¹ ; Liu Jiping ¹ ; Qin Zhaohai ¹ ;

作者机构： 1.China Agr Univ, Coll Sci, Beijing 100193, Peoples R China

2.Henan Acad Agr Sci, Zhengzhou 450002, Peoples R China

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.