Pyrifluquinazon类似物的设计、合成及杀虫活性  

Design,synthesis and insecticidal activity of pyrifluquinazon analogs

作　　者：王刚 梁爽 宋玉泉 英君伍 李斌 于海波 杨辉斌 WANG Gang;LIANG Shuang;SONG Yuquan;YING Junwu;LI Bin;YU Haibo;YANG Huibin(National Engineering Research Center of Pesticide,State Key Laboratory of the Discovery and Development of Novel Pesticide,Shenyang Sinochem Agrochemicals R&D Co.,Ltd.,Shenyang 110021,China)

机构地区：[1]沈阳中化农药化工研发有限公司新农药创制与开发国家重点实验室,农药国家工程研究中心,沈阳110021

出　　处：《农药》2024年第9期632-638,共7页Agrochemicals

摘　　要：[目的]寻找具有较高杀蚜虫活性的新化合物。[方法]以pyrifluquinazon为先导化合物,以3-(三氟甲基)-1H-1,2,4-三氮唑、4-氯-3-甲基-1H-吡唑和对氟硝基苯为起始原料,设计、合成了12个pyrifluquinazon类似物,并通过1H NMR和HRMS对其结构进行确证。[结果]初步活性测试结果显示,在100 mg/L剂量下,部分化合物对蚕豆蚜具有一定的杀虫活性,其中化合物13-5对蚕豆蚜的活性为97.2%,优于pyrifluquinazon(91.9%),化合物13-2对蚕豆蚜的活性大于80%。[Aims]This study aims to explore new compounds with high insecticidal activity against Aphis fabae.[Methods]Taking pyrifluquinazon as the lead compound,12 analogs of it were designed and synthesized with 3-(trifluoromethyl)-1H-1,2,4-triazole,4-chloro-3-methyl-1H-pyrazole and 4-fluoronitrobenzene as the initial materials.The compounds were confirmed by1H NMR and HRMS.[Results]The primarily test results showed that,some of the compounds displayed good insecticide activity against A.fabae at 100 mg/L.Among them,compound 13-5had an activity of 97.2%,which was better than that of pyrifluquinazo(91.9%),while compound 13-2 had an activity over 80%.

关 键 词：喹唑啉酮 杀虫活性 合成 

分 类 号：TQ450.11[化学工程—农药化工]