2,3a-二氢-苯并吡喃[4,3-c]吡唑-3-酮类衍生物的合成及其活性  

Synthesis and Activities of 2,3a-Dihydro-chromeno-[4,3-c]pyrazol-3-one Derivatives

作　　者：周中振[1,2] 陈琼[1] 杨光富 

机构地区：[1]华中师范大学农药与化学生物学教育部重点实验室,武汉430079 [2]南方医科大学药学院,广州510515

出　　处：《有机化学》2009年第11期1774-1783,共10页Chinese Journal of Organic Chemistry

基　　金：国家自然科学基金(Nos.20702018;20572030;20528201);国家973前期专项(No.2007CB11630);教育部跨世纪优秀人才;教育部重点科技项目(No.10420);湖北省自然科学基金优秀群体(No.2004ABC002)资助项目

摘　　要：为了进一步寻找新型黄酮类农药,以苯并吡喃[4,3-c]并吡唑-3-酮为先导结构,以4-氯苯甲醚为起始原料,设计合成了33种新型的2,3a-二氢-苯并吡喃[4,3-c]吡唑-3-酮类化合物,其结构经MS,HNMR和元素分析确证.并对化合1物7k的单晶进行了结构测定,对目标化合物进行了杀虫和杀菌活性测试.结果表明,大部分化合物显示出一定的杀菌活性和弱的杀虫活性.To search novel flavonoid pesticide, chromeno[4,3-c]pyrazol-3-ones were identified as lead compounds for further studies. And 33 novel 2,3a-dihydro-3a-methyl-chromeno[4,3-c]pyrazol-3-one derivatives were designed and synthesized using 1-chloro-4-methoxybenzene as starting material. The structures of the target compounds were determined by means of MS, 1H NMR and elemental analysis. The crystal structure of the target compound 7k was determined by X-ray diffraction analysis. At the same time, preliminary bioassay showed that most of target compounds showed feeble insecticidal activity but middling fungicidal activity.

关 键 词：苯并吡喃[4 3-c]吡唑 合成 杀虫活性 杀菌活性 

分 类 号：TQ450.21[化学工程—农药化工] O626.21[理学—有机化学]