新型5-[(3-甲基-5-(3,4)-二氯-1-苯基)]-吡唑基-(1,2,4)-三唑衍生物的设计合成研究  

The Design and Synthesis of Cyclohexane of 5-{[(3-methyl-5-chloro-1-(3,4)-dichloro phenyl)]-pyrazoly-(1,2,4)-triazolyl-[3,4]-1-sulfur-(3,4)-dinitrogen-5-[(3,5)dichloro-4-methyl)phenyl]-6-[(3-fluorination-4-nitro)phenyl]}

作　　者：陆阳[1] 陶京朝[2] 周志莲 张志荣[4] Lu Yang;Tao Jingzhao;Zhou Zhilian;Zhang Zhirong(Office of Organic chemistry,Xinyang Agriculture and forestry College,Xinyang Henan 464000,China;Chemistry Department of ZhengZhou University,Zhengzhou Henan 450001,China;New Drug Research and Development Center Henan KeYi Group,Xinyang Henan 464000,China;Henan FuBang Pesticides Chemical Engineering Company,Xinyang Henan 464000,China)

机构地区：[1]信阳农林学院有机化学教研室,河南信阳464000 [2]郑州大学化学系,河南郑州450001 [3]河南科易集团新药研究开发中心,河南信阳464000 [4]河南富邦农药化工公司,河南信阳464000

出　　处：《农药科学与管理》2021年第8期40-49,共10页Pesticide Science and Administration

摘　　要：根据拼合原理,将1-氯芳基-(3,4)-二氯苯基引入吡唑环设计成新颖结构的1-氯芳基-(3,4)-二氯苯基-4-(1,2,4)-三唑基吡唑化合物,并研究其合成工艺。寻求制备具有杀菌活性的化合物5-{[(3-甲基-5-氯-1-(3,4)-二氯苯基)]-吡唑基]-(1,2,4)-三唑-[3,4]-1-硫-(3,4)-二氮-5-[(3,5)-二氯-4-甲基)]苯基-6-[(3-氟-4-硝基)苯基]}环己烷。以3-甲基-(3,4)-二氯苯基-5-氯-5-吡唑啉酮和三氯氧磷为起始原料,经过氯甲酰化、氧化、酯化、肼解、取代、环合、缩合、亲核加成反应制得目标化合物5-{[(3-甲基-5-氯-1-(3,4)-二氯苯基)-吡唑基]-(1,2,4)-三唑-[3,4]-1-硫-(3,4)-二氮-5-[(3,5)-二氯-4-(甲基)苯基]-6-[(3-氟-4-硝基)-苯基]}环己烷。在优化的条件下,目标化合物纯度为99.1%。该工艺简单经济,条件温和,合成工艺减少了溶剂的用量和废物排放量。According to the principle of combination,1-aryl chloride-(3,4)-dichlorophenyl was introduced into pyrazole ring to obtain 1-aryl chloride-(3,4)-dichlorophenyl-4-(1,2,4)-triazole pyrazole compounds with novel structures.The synthesis process was studied to look for the compounds with fungicide activities.The target compounds can be obtained through chloroformylation,oxidation,esterification,hydrazinolysis,replace,cyclization,condensation and electeophilic addition reaction.3-methyl-(3,4)-dichloro-1--phenyl)-5-chlorination-5-pyrazolone and phosphorus oxychloride were used as raw materials.Under optimized conditions,the purity of the target compounds can reach up to 99.1%.The process is simple,economic and mild,reducing the amount of solvent and waste discharge.

关 键 词：吡唑环 合成 抑菌活性 

分 类 号：S482.2[农业科学—农药学]