杀菌剂丁香菌酯的创制经纬  

The Discovery of Fungicide Coumoxystrobin

作　　者：关爱莹[1] 刘长令[1] 李志念[1] 张明星[1] 司乃国[1] 

机构地区：[1]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

出　　处：《农药》2011年第2期90-92,共3页Agrochemicals

基　　金：国家重点基础研究发展规划"(973"计划)项目(2010CB126105)

摘　　要：概述了运用中间体衍生化方法发现杀菌剂丁香菌酯(SYP-3375)的过程:以取代香豆素环替换醚菌酯结构中的邻甲苯基,设计并合成了一系列化合物,发现先导化合物(反)-3-甲氧基-2-(2-((香豆素-7-基氧基)甲基)苯基)丙烯酸甲酯(3),通过优化研究发现SYP-2859、SYP-3200(甲香菌酯)等高活性化合物,最终发现了丁香菌酯,其对蔬菜和作物的多种病害如黄瓜霜霉病、黄瓜灰霉病、小麦白粉病、水稻纹枯病和苹果腐烂病等均有很好的防治效果,已于2010年获准临时登记。The discovery of fungicide coumoxystrobin（SYP-3375） was summarized by using the intermediate derivatization method.A series of compounds were designed and synthesized by the replacement of o-methylphenyl group of kresoxim-methyl with substituted coumarin moiety,the lead compound（E）-methyl 3-methoxy-2-（2-（（coumarin-7-yloxy）methyl）phenyl）acrylate（3） was discovered.SYP-2859 and SYP-3200（coumethoxystrobin） with higher activities were discovered continuously.Further optimization by structure-activity relationship study led to the discovery of coumoxystrobin（SYP-3375）,which has a broad spectrum fungicidal activity providing vegetable and crop protection from cucumber downy mildew,cucumber grey mold,wheat powdery mildew,rice sheath blight and apple valsa canker and was granted temporary registration in China in 2010.

关 键 词：中间体衍生化方法 丁香菌酯 杀菌活性 黄瓜霜霉病 苹果腐烂病 

分 类 号：TQ455.4[化学工程—农药化工]