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Position: Home > Articles > Design, Synthesis and Herbicidal Activity of Novel Sulfonylurea Derivatives Agrochemicals 2014 (12) 869-871

新型磺酰脲类化合物的设计、合成与除草活性

作  者:
柴宝山;孙旭峰;崔东亮;刘长令
单  位:
沈阳化工研究院有限公司新农药创制与开发国家重点实验室
关键词:
磺酰脲;嘧苯胺磺隆;合成;除草活性
摘  要:
[目的]利用中间体衍生化方法,设计合成一系列氨基磺酰脲类新化合物。[方法]以(取代)邻氨基苯甲酸为起始原料,通过与固体光气合环得到靛红酸酐,再与胺开环得到邻氨基苯甲酰胺中间体,最后再与嘧啶磺酰氯缩合得到磺酰脲类化合物。[结果]目标化合物结构经核磁表征。[结论]生物活性测定结果表明该类化合物具有较好的除草活性,可有效防除马唐和苘麻。并初步探讨了其结构活性关系。
译  名:
Design, Synthesis and Herbicidal Activity of Novel Sulfonylurea Derivatives
作  者:
CHAI Bao-shan;SUN Xu-feng;CUI Dong-liang;LIU Chang-ling;State Key Laboratory of the Discovery and Development of Novel Pesticide, Shenyang Research Institute of Chemical Industry Co., Ltd.;
关键词:
sulfonylurea;;orthosulfamuron;;synthesis;;herbicidal activity
摘  要:
[Aims] The study aims to design and synthesize a series of sulfonylurea derivatives using 'intermediate derivatization method' to discover herbicidal compounds with improved activity. [Methods] The intermediates of isatoic anhydride, which were prepared from(substituted) anthranilic acids and triphosgene, reacted with amines to obtain anthranilamides, and finally the target compounds of sulfonylurea derivatives were obtained by condensation of pyrimidine sulfamoyl chloride. [Results] Their structures were confirmed by 1H NMR. [Conclusions] Preliminary bioassay shows that the synthesized compounds have good herbicidal activities, which are effective to control of Digitaria sanguinalis and A b utilon the op hrasti. The relationship between structure and herbicidal activity is also reported.

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