论文部分内容阅读
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 process of derivatization of syringylcytosylate (SYP-3375) by an intermediate derivatization method was summarized. A series of compounds were designed and synthesized by substituting the coumarin ring for the o-tolyl group in the ester structure of kresoximde and found that the lead compound (3) Methyl (3-methoxy) -2- (2 - ((coumarin-7-yloxy) methyl) phenyl) acrylate was synthesized and the results showed that SYP- 3200 (toadstool) and other highly active compounds, culminating in the discovery of syringomycetin, which is harmful to vegetables and crop plants such as downy mildew, cucumber gray mold, wheat powdery mildew, rice sheath blight and apple rot Disease and so on have a very good control effect, was approved in 2010 temporary registration.