新型吡唑啉酮类化合物的合成及生物活性测定  

Synthesis and Biological Activity of Novel Pyrazolone Compounds

作　　者：杨莉[1] 李淼[2] 房晓敏[1] 陈伟[1] 程玉龙[1] 丁涛[1] 

机构地区：[1]河南大学化学化工学院精细化学与工程研究所,河南开封475004 [2]沈阳化工研究院有限公司新农药创制与开发国家重点实验室,沈阳110021

出　　处：《农药》2014年第6期399-401,452,共4页Agrochemicals

摘　　要：[目的]制备新型吡唑啉酮类化合物。[方法]以唑菌酯关键中间体3-(4-氯苯基)-1-甲基-1H-吡唑-5-醇为起始原料,经过羟醛缩合反应合成中间体4-(4-羟基-3-甲氧基苯亚甲基)-3-(4-氯苯基)-1-甲基-1H-吡唑-5(4H)-酮,再经亲核取代反应、酯化反应制备了11个新型吡唑啉酮类化合物。[结果]目标化合物的结构经过1H NMR进行了确证。[结论]室内生测结果表明该类化合物具有较好的杀菌和杀虫活性。[Aims] The study aims to prepare novel pyrazolone compounds. [Methods] The intermediate of novel pyrazolone compounds 4-（4-hydroxy-3-methoxybenzylidene）-3-（4-chlorophenyl）-1-methyl-1H-pyrazol-5（4H）-one was synthesized from 3-（4-chlorophenyl）-l-methyl-lH-pyrazol-5-ol which was the key intermediate of pyraoxstrobin via aldol reaction. Followed by furthernucleophilic substitution and esterification to obtain eleven novel pyrazolone compounds. [Results] All compounds were confirmed by 1H NMR. [Conclusions] The indoor test results showed that most of compounds had good bactericidal and insecticidal activity.

关 键 词：吡唑啉酮 合成 杀菌活性 杀虫活性 

分 类 号：O626[理学—有机化学]