含异噁唑环的新型2,5-二取代-1,3,4-噁二唑的合成及其杀菌活性

Synthesis and Fungicidal Activities of Novel 2,5-Disubstituted-1,3,4-oxadiazoles Containing Isoxazole Ring

以取代异噁唑甲酸乙酯为起始原料,经取代、加成与环化反应合成了5个新型2-取代苯胺基-5-(取代异噁唑-4-基)-1,3,4-噁二唑(5a～5e),产率54.0%～86.7%,其结构经1H NMR,IR和元素分析表征。初步杀菌活性试验表明,5a,5c和5d对番茄灰霉病菌有很高的抑制作用,其活性高于对照药剂多菌灵。

Five novel 2-substituted phenylamino-5-（substituted isoxazol-4-yl）-1,3,4-oxadiazoles（5a^5e） in yields of 54.0%~86.7% were synthesized from ethyl substituted isoxazol-4-yl formate by substitution,addition and cyclization reaction.The structures were characterized by 1H NMR,IR and elemental analysis.Preliminary fungicidal activity tests showed that 5a,5c and 5d exhibited good inhibitory activities against botrytis cinerea pers and the activities were higher than that of the control fungicide（carbendazim）.