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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 process of derivatizing the fungicide pyraclostrobin (SYP-3343) using an intermediate derivatization method is summarized. A series of compounds were designed and synthesized by substituting the substituted pyrazole ring for the coumarin ring in the syringalicylic ester structure. It was found that the lead compound (2), a number of highly active compounds were found through optimization studies and finally (E) -2- (2 - ((3- (4- chlorophenyl) Methoxy) methyl) phenyl) -3-methoxyacrylate, namely pyraclostrobin (SYP-3343), has a broad spectrum of bactericidal activity against various diseases of vegetables and crops such as downy mildew , Rice blast, powdery mildew and anthracnose, etc. SYP-3343 has obvious insecticidal and miticidal activities and can achieve the purpose of treating both pests and diseases. It was approved in 2009 for temporary registration.