除草剂NWAFU-J10创制经纬

Discovery of herbicide NWAFU-J10

以除草剂苯噻酰草胺、草除灵、苯噻隆和噻唑禾草灵中共有的苯并噻唑为起始原料,基于非活性基团多样化衍生策略,通过苯并噻唑3-位引入取代苯基和吡啶基构建化合物库。采用小杯法评价了所合成化合物对稗草和马齿苋的除草活性,发现先导化合物3-(3-氯-5-三氟甲基吡啶-2-基)苯并噻唑2-酮(化合物99)。再先导优化,最终获得具有3-吡啶基苯并噻唑-2-酮新颖分子骨架的高除草活性候选化合物NWAFU-J10。NWAFU-J10合成工艺简便、生产成本较低,对大多阔叶杂草表现出极高除草活性,具有良好产业化开发前景。

Based on the strategy of structural diversity-oriented inactive groups,a compound library was constructed by introducing a variety of substituted phenyls and pyridines at the 3-position of benzothiazole,the inactive group commonly found in the chemical structures of herbicides such as mefenacet,benazolin-ethyl,benzthiazuron and fenthiaprop-ethyl.The herbicidal activities of all compounds against barnyard grass and purslane were evaluated by using small cup method,and 3-(3-chloro-5-(trifluoromethyl)pyridin-2-yl)benzo[d]thiazol-2(3H)-one(99)was discovered as lead compound.After repeatedly structural optimization,the highly active herbicide candidate compound NWAFU-J10 was finally obtained.NWAFU-J10 features a novel molecular skeleton of 3-pyridylbenzothiazol-2-one,low production cost and convenient synthesis process.It exhibits extremely high herbicidal activity against most broadleaf weeds and has good prospects for industrial development.