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用苯异氰酸酯与胺反应,设计并合成了一个含除草剂敌草隆和灭草隆的25个脲类化合物库,用含异氰酸酯基团或胺基团的树脂对产物进行了提纯。按组合化学中的“索引”方法,此化合物库分为10个子库。用常规方法对10个子库进行除草活性筛选,依据子库除草活性的顺序,重新“发现”了除草剂敌草隆和灭草隆。在新农药创制中应用这种方法,可节省时间和工作。
A series of 25 urea compounds containing herbicides Diuron and Monuron were designed and synthesized by the reaction of benzene isocyanates with amines. The products were purified with resins containing isocyanate groups or amine groups. According to the “index” method in combinatorial chemistry, this compound library is divided into 10 sub-libraries. Ten sub-pools were screened for their herbicidal activity using conventional methods and “discovered” the herbicides diuron and imazamil again in the order of their herbicidal activity. Applying this approach to new pesticide creation saves you time and effort.