新型3-羟亚甲基吡咯烷-2,4-二酮衍生物的合成与除草活性研究

Synthesis and Herbicidal Evaluation of Novel 3-(Hydroxymethylene)pyrrolidine-2,4-dione

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19种酮酸酯与氨基酸酯合成了19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,IR和元素分析确证.初步生物活性测试结果表明,其生长抑制活性高于对照药HPPD抑制剂磺草酮.与已报道的高活性化合物相比,对油菜的抑制率明显得到提高,但对稗草的生长抑制没有明显的改善.

In order to further study the structure-activity relationships （SAR） of the title compounds and find new kinds of herbicides, nineteen new compounds were prepared by reaction of nineteen 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 their inhibiting rates were higher than sulcotrione. In comparison with the reported compounds with excellent herbicidal activity, their inhibiting rates against B. campestrisroot were elevated significantely while their inhibiting rates against E. crus-galli were not improved.