新磺酰脲类化合物的合成及生物活性

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.

Synthesis and Herbicidal Activity of New Sulfonylurea Derivatives

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..