摘要：A series of strobilurin-l,2,4-triazole derivatives containing a furan or thiophen ring was designed andsynthesized. The structures of the compounds were characterized by 1H NMR, 13C NMR and HRMS spectra. Thebioassays indicated that the fungicidal activities of compounds 10b（EC50=14.82 mg/L） and 10c（EC50=18.72 mg/L）against Cercospora arachidicola Hori in vitro were much higher than that of Azoxystrobin as control（EC50=40.54mg/L） and the fungicidal activities of compounds 10u（EC50=8.66 rag/L） and 10n（EC50=9.89 rag/L） against Rhizotoniacerealis in vitro were higher than that of the same control（EC50=10.86 rag/L）. Compounds 10b, 10c, 1011 and 10kcould be considered as the leading compounds for further investigation.

摘要：To discover novel strobilurins analogues with good and broad spectrum activity,a series of nove 3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-dioxides-based strobilurins was designed,synthesized,and tested agains various phytopathogenic *** *** 7k exhibited substantial and broad spectrum antifungal activities against the tested phytopathogenic fungi,especially compound 7b,which showed 100%,80%,90%,and 90%antifungal activity(in virto)against Erysiphe graminis(***),Puccinia sorghi Schw:(P sorghi Schw.)Colletotrichum lagenarium(***),and Pseudoperonospora cubensis(P cubensis)at 300 ug/mL,*** or comparable to the positive control ***,compound 7b exhibited 85%greenhouse *** activity(in vivo)against *** even at 0.2μg/mL,equal to azoxystrobin(90%)and trifloxystrobin(90%)Meanwhile,compound 7b against P cubensis displayed 70%and 55%greenhouse inhibition activity(in vivo)at 1.56 and 0.2μg/mL,respectively,much better than those of azoxystrobin and trifloxystrobin(both 0%at 1.56 and 0.2 ug/mL).Therefore,compound 7b could be considered as the most promising fungicidal candidate for furthe ***,based on the effective concentration(ECso)against ***,the built CoMSIA model provided the useful reference for the further structural optimization design.

摘要：以苯并五元环为基本结构对肟醚类strobilurin杀菌剂侧链进行修饰,共设计合成了13个结构新颖的肟醚类化合物.室内生物活性测试结果表明所合成的化合物对小麦白粉病(Eryiphe graminis)和黄瓜霜霉病(Pseudoperonospora cubensis)均具有优异的抑菌活性,而所合成的部分茚取代肟醚类化合物还具有广谱的杀虫活性.同时,用钯催化“一锅法”反应以较高的收率合成了关键中间体2-乙酰基茚衍生物.