| 杀螨剂嘧螨胺(SYP-11277)的创制经纬 |
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| 引用本文： | 柴宝山,刘长令,张弘,李慧超,罗艳梅,刘少武,宋玉泉.杀螨剂嘧螨胺(SYP-11277)的创制经纬[J].农药,2011,50(5). |
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| 作者姓名： | 柴宝山 刘长令 张弘 李慧超 罗艳梅 刘少武 宋玉泉 |
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| 作者单位： | 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,沈阳,110021 |
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| 基金项目： | 国家重点基础研究发展规划("973"计划)项目 |
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| 摘 要： | 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.
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| 关 键 词： | 中间体衍生化方法 先导发现 嘧螨胺 杀螨活性 杀卵活性 |
The Discovery of Acaricide SYP- 11277 |
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| CHAI Bao-shan,LIU Chang-ling,ZHANG Hong,LI Hui-chao,LUO Yan-mei,LIU Shao-wu,SONG Yu-quan.The Discovery of Acaricide SYP- 11277[J].Pesticides,2011,50(5). |
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| Authors: | CHAI Bao-shan LIU Chang-ling ZHANG Hong LI Hui-chao LUO Yan-mei LIU Shao-wu SONG Yu-quan |
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| Affiliation: | CHAI Bao-shan,LIU Chang-ling,ZHANG Hong,LI Hui-chao,LUO Yan-mei,LIU Shao-wu,SONG Yu-quan(State Key Laboratory of the Discovery and Development of Novel Pesticide,Shenyang Research Institute ofChemical Industry Co.,Ltd.,Shenyang 110021,China) |
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| Abstract: | The discovery of acaricide SYP-11277 was briefly reviewed in this paper.A series of compounds weresynthesized by chemical reaction from substituted pyrimidin-4-ol,and the lead compound 1 with acaricidal activitywas discovred(the discovery of lead compound by using the intermediate derivatization method).Further studythrough modification of the structure led to discover the lead compound 2,which was optimized to discover highactivities compounds SYP-10913,SYP-11277,SYP-11992 and SYP-11993.Finally,SYP-11277 w... |
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| Keywords: | intermediate derivatization method lead discovery SYP-11277 acaricidal activities ovicidal activities |
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