Synthesis and bioactivity of 2-(2-(1-substitued-1H-pyrazol-3-yl) phenoxy)-4, 6-dimethoxypyrimidine derivatives | 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的合成及其生物活性

Chinese. 寻找具有除草活性及抑菌活性的新型化合物。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。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%。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。

English. The purpose of the study was looking for the novel compounds with herbicidal activities and fungicidal activities. Novel 2-(2-(1-substitued-1H-pyrazol-3-yl)phenoxy)-4, 6-dimethoxyp yrimidine 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. Five novel 2-(2-(1-substitued-1H-pyrazol-3-yl)phenoxy)-4, 6-dimethoxypyrimi dine 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. 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.