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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 relationship of 3-hydroxymethylenepyrrolidine-2,4-dione compounds, in order to find out highly active compounds, the indole ring with aromaticity was introduced by the bioisosterism principle and 22 compounds were synthesized The novel 3-hydroxymethylene pyrrolidine-2,4-dione derivatives reported in the literature have been confirmed by1H NMR and elemental analysis.The preliminary bioassay results show that these compounds have certain herbicidal activity.Preliminary The structure-activity relationship studies showed that the herbicidal activity of pyrrolidine-2,4-dione compounds was related to the relative configuration of planes A and B.