【作者】 王立增； 冯聪； 朱敏娜； 兰杰； 孙旭峰； 关爱莹； 张金波； 刘长令； 杨新玲；

【Author】 WANG Li-zeng;FENG Cong;ZHU Min-na;LAN Jie;SUN Xu-feng;GUAN Ai-ying;ZHANG Jin-bo;LIU Chang-ling;YANG Xin-ling;State Key Laboratory of the Discovery and Development of Novel Pesticides, Shenyang sinochem agrochemicals R&D Co., Ltd.;Department of Applied Chemistry, College of Science, China Agricultural University;

【机构】 沈阳中化农药化工研发有限公司新农药创制与开发国家重点实验室； 中国农业大学理学院应用化学系；

【摘要】 [目的]含嘧啶环的农药作为一类重要的农药品种是农药研发的热点领域之一,以其优异的广谱杀菌杀虫杀螨活性引起广泛的关注。另外,嘧啶胺类商业化品种如氟嘧菌胺(杀菌剂),嘧虫胺(杀虫杀螨剂)表现出优异的植物保护活性。[方法]为了开发具有显著活性的嘧啶胺类化合物,本文利用中间体衍生化方法(IDM)设计合成了一系列含有苯环和吡啶环的新型芳基烷基胺类化合物,并进行了生物活性测试。目标化合物的结构均经过1HNMR,IR,MS和元素分析确认。[结果]其中化合物SYP-9069和SYP-2260表现出突出的生物活性,这两个化合物均具有广谱杀菌杀虫杀螨活性,SYP-9069对黄瓜霜霉病和白粉病具有优异防治效果,SYP-2260在较低剂量下对蚕豆蚜(LC50=0.1708 mg/L),桃蚜(LC50=0.2455 mg/L),棉蚜(LC50=0.2632mg/L)和朱砂叶螨(LC50=0.8892mg/L)展现出优异防治效果。田间验证试验中两个化合物与现有商品化品种相比也表现出优异活性。生测结果表明SYP-9069和SYP-2260可作为先导化合物进行深入研究以发现可供开发的新型嘧啶胺类农药品种。更多还原

【Abstract】 The pesticides containing pyrimidine are known as one of the most important classes of agrochemicals with broad spectrum fungicidal,insecticidal and/or acaricidal activities.Furthermore,the pyrimidinamine derivatives such as diflumetorim（fungicide）,flufenerim（insecticide and acaricide）display excellent bioactivities as crop protection produccts.[Methods]To discover new pyrimidine analogues with improved activities,employing the intermediate derivatization method（IDM）,a series of novel pyrimidine derivatives containing alkylamine substituted with phenyl and pyridine were synthesized and bioassayed.The title compounds were identified by 1 H NMR,IR,MS and elemental analysis.[Results]Among them the activities of two compounds,SYP-9069 and SYP-2260,showed outstanding activities.They both exhibited broad-spectrum bactericidal,insecticidal,and acaricidal activities,particularly,SYP-9069 showed excellent control against cucumber downy mildew and powdery mildew,SYP-2260 showed good control against black bean aphid(LC₅₀=0.1708 mg/L),green peach aphid(LC₅₀=0.2455 mg/L),cotton aphid(LC₅₀=0.2632 mg/L),Tetranychus cinnabarinus(LC₅₀=0.8892 mg/L)at a lower dosage.The present work demonstrates that SYP-9069 and SYP-2260 can be used as possible lead compounds for further developing novel pesticides.更多还原