摘要
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 25 member library of ureas including the commercial herbicides Monuron and Diuron was generated by reacting 6 mmol of the isocyanate with a mixture containing 1 mmol each of the five amines and 6 mmol of the amine with a mixture containing 1 mmol each of the five isocyanate. The library was purified by resins containing isocyanate or amine group to scavenge the excess amines or isocyanates. Each of the 25 compounds in the library was prepared twice, as a component of two different pools. The ten pools were screened by the conventional procedures. The herbicides Monuron and Diuron are successfully rediscovered'. It seems that the indexed' combinatorial strategy is a useful tool to find a potent compound rapidly in a particular area of chemistry.
出处
《农药》
CAS
北大核心
1999年第5期16-18,共3页
Agrochemicals
关键词
脲类化合物库
液相合成
除草剂
除草活性
synthesis, urea library,resin,combinatorial,chemistry,agrochemical discovery.
