新型3-(α-羟基吲哚亚甲基)吡咯烷-2,4-二酮衍生物的合成与除草活性研究  

Synthesis and Bioactivities of Novel 3-α-Hydroxy(indol-3-yl)-methylene-pyrrolidine-2,4-dione Derivatives

作　　者：朱有全[1] 朱然[1] 袁燕伟[1] 张金[1] 王文虎[1] 邹小毛[1] 胡方中[1] 刘向明[1] 杨华铮[1] 

机构地区：[1]南开大学元素有机化学研究所元素有机化学国家重点实验室,天津300071

出　　处：《有机化学》2010年第8期1207-1211,共5页Chinese Journal of Organic Chemistry

基　　金：国家重点基础研究发展规划(No.2010CB126103);国家自然科学基金(No.20772066);教育部博士点新教师基金(No.20070055040)资助项目

摘　　要：为了进一步研究3-羟亚甲基吡咯烷-2,4-二酮类化合物构效关系,以期发现高活性化合物,利用生物等排原理引入具有芳香性的吲哚环,合成了22个未见文献报道的新型3-羟亚甲基吡咯烷-2,4-二酮衍生物,其结构均经过1HNMR和元素分析确证.初步生物活性测试结果表明,这些化合物均具有一定的除草活性.初步的构效关系研究表明,该类吡咯烷-2,4-二酮类化合物的除草活性与平面A和B的相对构型有关.In order to further study the structure-activity relationships of the title compounds and find new kinds of herbicides,the aromatic indole ring was introduced and 22 new compounds were prepared by reaction of ketoacid esters with amio-acid esters.All of them have been confirmed by 1H NMR spectra and elemental analysis.The preliminary bioassay results indicated that all of them possessed some extent herbicidal activities.Preliminary quantitative structure-activity relationship （QSAR） analysis indicated that the herbicidal activity for pyrrolidine-2,4-dione derivatives was strongly related with the configuration for planes A and B.

关 键 词：吲哚 吡咯烷-2 4-二酮 合成 除草活性 构效关系 

分 类 号：O626[理学—有机化学]