含嘧啶硫醚的嗜球果伞素类化合物的设计、合成及杀菌活性  

Design,synthesis and fungicidal activity of strobilurins containing pyrimidine thioether units

作　　者：郝树林 蔡增飞 曹杨羊 杜晓华 HAO Shulin;CAI Zengfei;CAO Yangyang;DU Xiaohua(Catalytic Hydrogenation Research Center,Zhejiang University of Technology,Zhejiang Key Laboratory of Green Pesticides and Cleaner Production Technology,Zhejiang Green Pesticide Collaborative Innovation Center,Hangzhou 310014,China)

机构地区：[1]浙江工业大学催化加氢中心,浙江省绿色农药清洁生产技术研究重点实验室,浙江省绿色农药协同创新中心,杭州310014

出　　处：《农药学学报》2021年第1期60-68,共9页Chinese Journal of Pesticide Science

基　　金：国家重点研发计划(2016YFD0300708).

摘　　要：为了发现和开发新的杀菌化合物,以嘧菌酯为先导,通过活性亚结构拼接等手段,设计并合成了22个新化合物,通过核磁共振氢谱、碳谱及高分辨质谱等手段对其结构进行了表征。生物活性测试结果表明,部分化合物对黄瓜白粉病菌表现出较好的杀菌活性,其中化合物7b在50 mg/L下对黄瓜白粉病菌的抑制率为85%。田间试验结果显示,在有效成分281.25 g/hm^(2)剂量下,化合物7b对黄瓜白粉病的防治效果与商品化品种推荐使用剂量时嘧菌酯(有效成分281.25 g/hm^(2))和乙嘧酚(有效成分300.00 g/hm^(2))的防治效果相当。To discover and exploit novel fungicidal compounds,twenty two novel strobilurin derivatives were designed and synthesized by sub-structural combination method using azoxystrobin as the lead compound.Their structures were characterized by 1H NMR,13C NMR and HRMS.Some compounds exhibited high fungicidal activity against Sphaerotheca fuliginea.In greenhouse tests,compound 7b displayed 85%fungicidal activity against cucumber powdery mildew at 50 mg/L.In field trials,compound 7b(281.25 g a.i./hm^(2))for cucumber powdery mildew proved to be approximately equivalent to commercial products azoxystrobin(281.25 g a.i./hm^(2))and ethirimol(300.00 g a.i./hm^(2)).

关 键 词：嗜球果伞素 嘧啶硫醚 新农药合成 杀菌活性 

分 类 号：O626.2[理学—有机化学] TQ455.4[理学—化学]