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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
引用本文:朱有全,司学凯,邹小毛,刘斌,杨华铮. 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[J]. 有机化学, 2007, 27(3): 385-390
作者姓名:朱有全  司学凯  邹小毛  刘斌  杨华铮
作者单位: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
基金项目:国家重点基础研究发展计划(973计划)(No.2003CB11l4400)、国家自然科学基金(No.20572054)和国家高等教育博士点基金资助项目
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1H NMR, 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.

关 键 词:除草剂  对羟基苯基丙酮酸双氧化酶  吡咯烷
收稿时间:2006-06-28
修稿时间:2006-06-28

Synthesis and Herbicidal Evaluation of Novel 3-(Hydroxymethylene)pyrrolidine-2,4-dione
ZHU You-Quan,SI Xue-Kai,ZOU Xiao-Mao,LIU Bin,YANG Hua-Zheng. Synthesis and Herbicidal Evaluation of Novel 3-(Hydroxymethylene)pyrrolidine-2,4-dione[J]. Chinese Journal of Organic Chemistry, 2007, 27(3): 385-390
Authors:ZHU You-Quan  SI Xue-Kai  ZOU Xiao-Mao  LIU Bin  YANG Hua-Zheng
Affiliation:State Key Laboratory of Elemento-organic Chemistry, Institute of Elemento-organic Chemistry, Nankai University, Tianjin 300071
Abstract: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 pre- liminary 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. campestris- root were elevated significantely while their inhibiting rates against E. crus-galli were not improved.
Keywords:herbicide  p-hydroxyphenypyruvate dioxydenase  pyrrolidine
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