| 吴文能,费强,何军,欧阳贵平.化学通报,2019,82(1):74-79. |
| 含2-甲基-4胺基嘧啶结构的1,3,4-噁二唑(噻二唑)硫醚化合物的合成及抗菌活性研究 |
| Synthesis and Biological Activity of 1,3,4- Oxadiazole(Thiadiazole) Thioether Derivatives Containing 2-methylp-4-amineyrimidine Moiety |
| 投稿时间：2018-08-07 修订日期：2018-08-23 |
| DOI： |
| 中文关键词: 嘧啶 1,3,4-噁二唑 1,3,4-噁二唑(噻二唑) 杀菌 合成 |
| 英文关键词:pyrimidine 1,3,4-oxadiazol,1,3,4-thiadiazole fungicide synthesis |
| 基金项目:贵州省自然科学基金项目(黔科合基础[2016]1006)；贵阳市科技局贵阳学院专项(GYU-KYZ[2018]01-09)；大学生创新创业训练计划项目(2018520835)资助 |
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| 中文摘要: |
| 以2-甲基-4-氨基-5-氰基嘧啶为原料,通过水解、酯化、肼解、环化和醚化等步骤,合成了12个含1,3,4-噁二唑(噻二唑)取代嘧啶化合物。通过1H NMR,13C NMR,MS 和元素分析进行确证其结构。初步抑菌活性测试标明,化合物浓度在50 μg/mL时,化合物6f和6f′对油菜菌核病菌(S. sclerotiorum)、马铃薯晚疫病菌(P. infestans)、水稻纹枯病(T. cucumeris)、小麦赤霉病菌(G. zeae)具有中等抑制率,其活性与对照药剂醚菌酯相当。 |
| 英文摘要: |
| Based on 4-amino-2-methylpyrimidine-5-carbonitrile as raw material, twelve 2-methyl-5-(5-
substitutional-1,3,4-oxadiazol/thiadiazole-3-yl)pyrimidin-4-amine compounds were synthesized through five step reactions including hydrolysis, esterification, hydrazidation, cyclization and thioetherification. The structures of title compounds were characterized by 1H NMR, 13C NMR, MS and elemental analysis. Preliminary bioassay results showed that the compounds 6f and 6f′ had moderate inhibitory activities against S. sclerotiorum, P. infestans, T. cucumeris and G. zeae at the concerntration of 50 μg/mL, Which were similar to that of Azoxystrobin. |
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