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概述了杀螨剂嘧螨胺(SYP-11277)的创制经纬。首先以取代嘧啶醇为中间体进行衍生化研究,合成了一系列化合物,从而发现了具有杀螨活性的先导化合物1(运用中间体衍生化方法发现先导化合物),然后通过结构修饰发现二次先导化合物2,进一步优化研究发现SYP-10913、SYP-11277、SYP-11992、SYP-11993等高活性化合物,最终确定嘧螨胺(SYP-11277)作为候选杀螨剂进行产业化开发。该药剂对红蜘蛛成、若、幼螨均具有很好的防治效果,而且表现了优异的杀卵活性。
An overview of the creation of the acaricide mite mite fungal (SYP-11277) creation latitude and longitude. First, the derivatization of substituted pyrimidinols was studied, and a series of compounds were synthesized. As a result, the lead compound 1 with acaricidal activity was found (the lead compounds were found by derivatization of intermediates), and then the secondary leads were found through structural modification Compound 2 was further optimized to find SYP-10913, SYP-11277, SYP-11992, SYP-11993 and other highly active compounds, and the pyrimidarone (SYP-11277) was finally identified as a candidate acaricide for industrial development. The agent on the red spider into, if, young mites have good control effect, but also showed excellent ovicidal activity.