1,2,4-三嗪酮类衍生物的合成研究及生物活性测试

Synthesis and Fungicidal Activities of 1,2,4-Triazinone Derivatives

以5-甲基-1,3,4-二唑-2(3H)-酮为原料,经过烷基化、扩环、水解和酰胺化等4步反应合成了12个新型的1,2,4-三嗪酮类化合物6a～6l,其结构经1H NMR、13C NMR和MS表征。初步生物活性测试结果表明,在50 g/mL质量浓度下,部分目标化合物对小麦赤霉病菌、辣椒枯萎病菌和苹果腐烂病菌表现出一定的生物活性。

Using 5-methyl-l,3,4-oxadiazol-2（3H）-one as starting material, twelve novel 1,2,4-triazinone derivatives were synthesized through alkylation, ring-enlargement, hydrolysis and amidation. All title compounds were characterized by 1H NMR, 13C NMR and MS. The preliminary bioassay indicated that some of the compounds exhibited certain fungicidal activities against Gibberella zeae, Fusarium oxysporum and Cytospora mandshurica at a dosage of 50 μg/mL.