摘要
以正在开发的新磺酰脲类除草剂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 1H NMR谱及元素分析确证.盆栽试验和离体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.
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 ALS screening 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..
出处
《高等学校化学学报》
SCIE
EI
CAS
CSCD
北大核心
2003年第9期1599-1603,共5页
Chemical Journal of Chinese Universities
基金
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
