| 杀菌剂唑菌酯的创制经纬 |
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| 引用本文： | 李淼,刘长令,李志念,李林,张弘,司乃国.杀菌剂唑菌酯的创制经纬[J].农药,2011,50(3). |
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| 作者姓名： | 李淼 刘长令 李志念 李林 张弘 司乃国 |
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| 作者单位： | 沈阳化工研究院有限公司,新农药创制与开发国家重点实验室,沈阳,110021 |
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| 基金项目： | 国家重点基础研究发展规划(“973”计划)项目(2010CB126105) |
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| 摘 要： | 概述了运用中间体衍生化方法发现杀菌剂唑菌酯(SYP-3343)的过程:以取代吡唑环替换丁香菌酯结构中的香豆素环,设计并合成了一系列化合物,发现先导化合物(2),通过优化研究发现多个高活性化合物,最终发现了(E)-2-(2-((3-(4-氯苯基)-1-甲基-1H-吡唑-5-基氧基)甲基)苯基)-3-甲氧基丙烯酸甲酯,即唑菌酯(SYP-3343),其具有广谱的杀菌活性,对蔬菜和作物的多种病害如霜霉病、稻瘟病、白粉病、炭疽病等均有很好的防治效果,同时SYP-3343具有明显的杀虫、杀螨活性,可达到病虫兼治之目的。已于2009年获准临时登记。
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| 关 键 词： | 中间体衍生化方法 唑菌酯 杀菌活性 霜霉病 |
The Discovery of Fungicide Pyraoxystrobin |
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| LI Miao,LIU Chang-ling,LI Zhi-nian,LI Lin,ZHANG Hong,SI Nai-guo.The Discovery of Fungicide Pyraoxystrobin[J].Pesticides,2011,50(3). |
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| Authors: | LI Miao LIU Chang-ling LI Zhi-nian LI Lin ZHANG Hong SI Nai-guo |
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| Affiliation: | LI Miao,LIU Chang-ling,LI Zhi-nian,LI Lin,ZHANG Hong,SI Nai-guo(State Key Laboratory of the Discovery and Development of Novel Pesticide,Shenyang Research Institute of Chemical Industry Co.Ltd.,Shenyang 110021,China) |
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| Abstract: | The discovery of fungicide pyraoxystrobin(SYP-3343) was reviewed by using the intermediate derivatization method.A series of compounds were designed and synthesized by the replacement of coumarin group of coumoxystrobin with substituted pyrazole moiety,the lead compound(2) was discovered.Further optimization by structure-activity relationship study led to the discovery of methyl(E)-2-(2-((3-(4-chlorophenyl)-1-methyl-1H-pyrazol-5-yloxy)methyl)phenyl)-3-methoxyacrylate(pyraoxystrobin,SYP-3343),which has a bro... |
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| Keywords: | intermediate derivatization method pyraoxystrobin fungicidal activities downy mildew |
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