| 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-(2-硝基苯基)乙腈为原料，经缩合、氧化、还原、环化、取代5步反应，合成了5-(4,6-二甲氧基嘧啶-2-基)-1-取代-3,5-二氢苯并［e］［1,4］氧氮杂卓-2(1H)酮类化合物，对合成的化合物进行核磁共振谱(1H NMR)、质谱(MS)及元素分析，并分别测定合成衍生物的除草活性及抑菌活性。【结果】经1H NMR、MS及元素分析确认，成功合成了15个新型的5-(4,6-二甲氧基嘧啶-2-基)-1-取代-3,5-二氢苯并［e］［1,4］氧氮杂卓-2(1H) 酮类化合物5和6a～6n。生物活性试验结果表明，在450 g/hm2的剂量条件下，目标化合物5、6a、6b和6c对芥菜，6m和6n对芥菜、反枝苋及小藜显示出30%～40%的除草活性。在200 mg/L的质量浓度下，目标物6c、6h和6m对黄瓜白粉病表现出30%以上的抑菌活性。【结论】本研究合成的化合物具有一定的除草和抑菌活性，其结构具有进一步改造研究的价值。 |
| 关键词: 4,6-二甲氧基嘧啶 ［1,4］氧氮杂卓酮 除草活性 抑菌活性 |
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| 基金项目:湖南省科技计划项目(2012NK3098)；湖南省教育厅科学研究重点项目(11A092)；怀化市科技计划项目(2013) |
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| Synthesis and bioactivity of a series of 4,6-dimethoxypyrimidin derivatives |
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| Abstract: |
| 【Objective】The purpose of the study was to synthesize novel compounds with herbicidal and fungicidal activities. 【Method】Fifteen novel 5-(4,6-dimethoxypyrimidin-2-yl)-1-substituted-3,5-dihydrobenzo［e］［1,4］oxazepin-2(1H)-one derivative compounds were synthesized using 2-(2-nitrophenyl)acetonitrile as starting material through five steps,including condensation,oxidation,reduction,cyclization and substitution reactions.All synthesized compounds were confirmed by 1H NMR,MS and elemental analysis techniques.The herbicidal and fungicidal activities of the new compounds were determined.【Result】Fifteen novel 5-(4,6-dimethoxypyrimidin-2-yl)-1-substituted-3,5-dihydrobenzo［e］［1,4］ oxazepin-2(1H)-one derivative compounds were synthesized.Preliminary biological activity test showed that target compounds 5,6a,6b,6c,6m and 6n exhibited 30%-40% herbicidal activities against Brassica juncea,Amaranthus retroflexus and Chenopodium serotinum L.at 450 g/hm2,while target compounds 6c,6h and 6m exhibited more than 30% fungicidal activities against Sphaerotheca fuliginea at 200 mg/L.【Conclusion】The compounds synthesized in this study had good potential and should be further studied. |
| Key words: 4,6-dimethoxypyrimidine ［1,4］oxazepin one herbicidal activity fungicidal activity |
