1-甲基-1H-吡唑-5-甲酰胺类化合物的合成与生物活性研究  

Synthesis and Biological Activities of 1-Methyl-1H-pyrazole-5-carboxamide Derivatives

作　　者：王二龙[1,2,3] 马保德[2,3] 柳爱平[2,3] 刘民华[2,3] 胡礼[2,3] 李微[2,3,4] 李建明[2,3] 高德良[2,3] 兰支利[1] 黄明智[2,3] 

机构地区：[1]湖南师范大学化学化工学院,湖南长沙410081 [2]湖南化工研究院有限公司国家农药创制工程技术研究中心,湖南长沙410014 [3]农用化学品湖南省重点实验室,湖南长沙410014 [4]长沙理工大学化学与生物工程学院,湖南长沙410004

出　　处：《精细化工中间体》2015年第5期5-9,共5页Fine Chemical Intermediates

基　　金：国家自然基金资助项目(21272062)

摘　　要：以丁酮、草酸二乙酯为原料,经Claisen缩合、Knorr环合和甲基化等多步反应合成了8个结构新颖的1-甲基-1H-吡唑-5-甲酰胺类化合物,其结构经Mass和1H NMR等确证。生测结果表明:化合物7a和7g在200 mg/L浓度下,对蚜虫表现出95%以上的活性;而化合物7h在100 mg/L浓度下,对小麦白粉病菌具有73.8%的防治效果。The eight novel 1-methyl-lH-pyrazole-5-carboxamide derivatives were synthesized in a multi-step process involving Claisen condensation, Knorr cyclization and methylation by using butanone and diethyl oxalate as raw materials and their structures were confirmed by MS and 1H NMR spectra. The preliminary bioassays indicated that the compounds 7a and 7g exhibited insecticidal more than 95% activity against Aphis at 200 mg/L. Compound 7h showed fungicidal activity against Erysiphe graminis were 73.8% at 100 mg/L.

关 键 词：吡唑酰胺 合成 生物活性 

分 类 号：S482.3[农业科学—农药学]