| 摘要: |
| 【目的】寻找具有除草活性及抑菌活性的新型化合物。【方法】以2-羟基苯乙酮为原料，经缩合、环化、选择性氮烷基化、氧取代4步反应合成了2-(2-(1-取代-1H-吡唑-3-基)苯氧基)-4,6-二甲氧基嘧啶类化合物，其结构运用1H NMR、MS和元素分析进行确认，并分别测定了合成化合物的除草活性及抑菌活性。【结果】经1H NMR、MS和元素分析确认，成功合成了5种新型的2-(2-(1-取代-1H-吡唑-3-基)苯氧基)-4,6-二甲氧基嘧啶类化合物。在150 g/hm2的剂量条件下，新合成化合物没有表现出除草活性；在200 mg/L的质量浓度条件下，化合物4,6-二甲氧基-2-(2-(1-丙基-1H-吡唑-3-基)苯氧基)嘧啶对黄瓜白粉病菌与水稻纹枯病菌的抑菌活性分别为78%和90%。【结论】2-(2-(1-取代-1H-吡唑-3-基)苯氧基)-4,6-二甲氧基嘧啶类化合物具有一定的抑菌活性，该类化合物的结构改造与修饰值得进一步研究。 |
| 关键词: 4,6-二甲氧基嘧啶 有机合成 生物活性 |
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| 基金项目:湖南省自然科学基金项目(09JJ6023)；湖南师范大学化学生物学及中药分析教育部重点实验室开放基金项目(KLCBTCMR2008-05)；怀化市科技计划项目(20093109) |
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| Synthesis and bioactivity of 2-(2-(1-substitued-1H-pyrazol-3-yl)-phenoxy)-4,6-dimethoxypyrimidine derivatives |
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| Abstract: |
| 【Objective】The purpose of the study was looking for the novel compounds with herbicidal activities and fungicidal activities.【Method】Novel 2-(2-(1-substitued 1H-pyrazol-3-yl)phenoxy)-4,6-dimethoxypyrimidine derivative compounds were synthesized using 1-(2-hydroxyphenyl)ethanone as starting material by condensation reaction,cyclization reaction,selective N-alkylate reaction and O-substitute reaction.All synthesized compounds were confirmed by 1H NMR,MS and elemental analysis techniques.Herbicidal activities and fungicidal activities of the new compounds were determined.【Result】Five novel 2-(2-(1-substitued-1H-pyrazol-3-yl)phenoxy)-4,6-dimethoxypyrimidine derivative compounds were synthesized.Synthetical compounds did not show herbicidal activities at 150 g/hm2.The antibacterial activity test indicated that 4,6-dimethoxy-2-(2-(1-propyl-1H-pyrazol-3-yl)phenoxy)pyrimidine (5 d) showed 78% and 90% inhibitory activities against Sphaerotheca fuliginea and Rhizoctonia solani respectively at 200 mg/L.【Conclusion】2-(2-(1-substitued-1H-pyrazol-3-yl)phenoxy)-4,6-dimethoxypyrimidine derivative compounds showed certain fungicidal activities.Therefore the structure’s modification of 4,6-dimethoxypyrimidine derivative compounds was worth further research. |
| Key words: 4,6-dimethoxypyrimidine organic synthesis bioactivity |
