2-取代硫醚-5-(5,7-二甲基-1,2,4-三唑并[1,5-a]嘧啶基)-1,3,4-噁二唑/噻二唑类化合物的合成及生物活性

以5-氨基-1H-1,2,4-三唑-3-羧酸乙酯为起始原料, 设计合成了11个新型的2-取代硫醚-5-(5,7-二甲基-1,2,4-三唑并1,5-a]嘧啶基)-1,3,4-噁二唑类化合物(5)和6个新型的2-取代硫醚-5-(5,7-二甲基-1,2,4-三唑并1,5-a]嘧啶基)-1,3,4-噻二唑类化合物(8). 通过¹H NMR, MS和元素分析对所合成的化合物进行了结构表征. 初步的生物活性测试结果表明, 所合成的化合物均表现出不同程度的除草及杀菌活性, 其中化合物5k和8f的活性最好, 在50 mg/L浓度下对水稻纹枯病菌的抑制率达90%以上.

Synthesis and Biological Activities of 2-Alkylthio-5-(5,7-dimethyl- 1,2,4-triazolo[1,5-a]pyrimidine-5-yl)-1,3,4-oxadiazole/ 1,3,4-thiadiazole Derivatives

Eleven novel 2-alkylthio-5-(5,7-dimethyl-1,2,4-triazolo1,5-a]pyrimidine-5-yl)-1,3,4-oxadiazole derivatives (5) and six novel 2-alkylthio-5-(5,7-dimethyl-1,2,4-triazolo1,5-a]pyrimidine-5-yl)-1,3,4-thia- diazole derivatives (8) have been designed and synthesized by using 5-amino-3-ethoxycarbonyl-1H-1,2,4- tri-azole as a starting material. All compounds synthesized were confirmed by ¹H NMR, MS spectra and elemental analyses. Preliminary bioassay indicates that some compounds display herbicidal ac-tivity and excellent fungicidal activity to some extent, and among them the compounds 5k and 8f b> exhibit higher than 90% inhibition effect against Rhizoctonia solani in dosage of 50 mg/L.