新型含吡唑环的N-甲氧基氨基甲酸甲酯类化合物的设计、合成及生物活性

以苯(吡啶)乙/丙酮类化合物为原料, 经酯化、环化和缩合三步制得新型含吡唑环的N-甲氧基氨基甲酸甲酯类化合物3a~3r, 化合物及其中间体的化学结构经红外光谱、核磁共振谱及元素分析确认. 生物活性结果表明, 化合物3在400 mg/L下分别对水稻稻瘟病、黄瓜霜霉病和小麦白粉病具有很好的防治效果. 对水稻稻瘟病, R₁为甲基或甲氧基取代的苯基时活性最好; 对于黄瓜霜霉病和小麦白粉病, R₁为苯基或甲基取代苯基的化合物杀菌活性优于其它化合物, R₂为甲基的化合物杀菌活性优于R₂为氢的化合物.

Design, Synthesis and Bioactivity of New N-Methoxycarbamate Containing Pyrazole

Strobilurins are one of the most important classes of agricultural fungicides. To discover new strobilurin analogues with high pesticidal activity, a series of new N-methoxycarbamate derivatives containing substituted pyrazoles 3a—3r were synthesized from substituted aryl alkyl ketones as starting material by esterification, cyclization and condensation. The structures of substituted pyrazole derivatives were confirmed by 1H NMR, IR and elemental analysis. Preliminary biological evaluation show that compounds 3 have good fungicidal activity against P. oryzae, P. cubensis and E. graminis at 400 mg/L. The compounds with R1=methyl or methoxy substituted phenyl have best activities against P. oryzae. The compounds with R1=phenyl or methyl substituted phenyl have higher activities against P. cubensis and E. graminis than the others and the compounds with R2=methyl have higher activities against fungi than that with hydrogen.