高等学校化学学报 ›› 2003, Vol. 24 ›› Issue (9): 1599.

• 论文 • 上一篇    下一篇

新磺酰脲类化合物的合成及生物活性

野国中, 范志金, 李正名, 李永红, 高发旺, 王素华   

  1. 南开大学和天津大学联合研究院, 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
  • 收稿日期:2002-08-30 出版日期:2003-09-24 发布日期:2003-09-24
  • 通讯作者: 李正名(1931年出生),男,教授,博士生导师,中国工程院院士,主要从事有机化学和农药化学领城的研究.E-mail:zml@nankai.edu.cn E-mail:zml@nankai.edu.cn
  • 基金资助:

    国家“八六三”项目(批准号:2001AA235011);教育部南开大学和天津大学科技合作基金;国家自然科学基金(批准号:20107003);教育部高等学校重点实验室访问学者基金

Synthesis and Herbicidal Activity of New Sulfonylurea Derivatives

YE Guo-Zhong, FAN Zhi-Jin, LI Zheng-Ming, LI Yong-Hong, GAO Fa-Wang, WANG Su-Hua   

  1. Joint Institute of Nankai University and Tianjin University, State Key Laboratory of Elemento-Organic Chemistry, Institute of Elemento-Organic Chemistry, Nankai University, Tianjin 300071, China
  • Received:2002-08-30 Online:2003-09-24 Published:2003-09-24

摘要: 以正在开发的新磷磺酰脲除草剂N-[2′-(4′-甲基)嘧啶基]-2-硝基苯磺酰脲的研究为基础,设计合成了19个脲桥经修饰的磺酰脲类化合物以及3个新型嘧啶中间体,产物结构经1HNMR谱及元素分析确证.盆栽试验和离休ALS酶研究结果表明,所合成的化合物均表现出一定的除草活性,部分化合物的除草活性较好.

关键词: 磺酰脲, 氨基嘧啶, 合成, 除草活性

Abstract: The sulfonylurea herbicides have been characterized by broad-spectrum of weed control at ultra-low dosage of application, good crop selectivity and low mammalian toxicity. Because of its high herbicidal activity, phototoxicity of sulfonylurea herbicides residues to succeeding crops and weed resistance has become the very important factors affecting its further development in China. In order to search for more environmental-benign sulfonylurea herbicides and study their structure-activity relationship, on the basis of study on a new sulfonylurea herbicide N-[(4'-methyl) pyrimidin-2'-yl]-2-nitro-phenylsulfonyl urea, also called monosulf uron, under commercialization in China, 19 novel sulfonylurea compounds modified at the bridge of urea and 3 related aminopyrimidines were synthesized. The structures of all compounds synthesized were confirmed by elemental analysis and 1H NMR. Preliminary herbicidal activity of the new sulfonylurea compounds derived from sulfonylurea bridge was determined by ALSscreening in vitro and pot bioassay experiment (in vivo). The results indicate that some compounds show good activities against ALS in vitro from Pisum sativum L. and Brassica napus L..

Key words: Sulf onylurea, Aminopyrimidine, Synthesis, Herbicidal activity

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