杀菌剂唑菌酯的创制经纬

The Discovery of Fungicide Pyraoxystrobin

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。

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 broad spectrum fungicidal activity providing vegetable and crop protection from downy mildew,rice blast,powdery mildew,anthracnose and so on.SYP-3343 also showed insecticidal and acaricidal activities,which enable it to control plant diseases and pest insects at the same time.SYP-3343 was granted temporary registration in China in 2009.