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中氮茚吡啶并[1,2-a]嘧啶酮类:三氟米唑嘧啶作为一种高效飞虱杀虫剂的发现。

Mesoionic pyrido[1,2-a]pyrimidinones: Discovery of triflumezopyrim as a potent hopper insecticide.

作者信息

Zhang Wenming, Holyoke Caleb W, Pahutski Thomas F, Lahm George P, Barry James D, Cordova Daniel, Leighty Robert M, Singh Vineet, Vicent Daniel R, Tong My-Hanh T, Hughes Kenneth A, McCann Stephen F, Henry Yewande T, Xu Ming, Briddell Twyla A

机构信息

DuPont Crop Protection, Stine-Haskell Research Center, 1094 Elkton Road, Newark, DE 19711, USA.

DuPont Crop Protection, Stine-Haskell Research Center, 1094 Elkton Road, Newark, DE 19711, USA.

出版信息

Bioorg Med Chem Lett. 2017 Jan 1;27(1):16-20. doi: 10.1016/j.bmcl.2016.11.042. Epub 2016 Nov 16.

Abstract

A novel class of mesoionic pyrido[1,2-a]pyrimidinones has been discovered with exceptional insecticidal activity controlling a number of insect species. In this communication, we report the part of the optimization program which led to the discovery of triflumezopyrim as a highly potent insecticide controlling various hopper species. Our efforts in discovery, synthesis, structure-activity relationship elucidation, and biological activity evaluation are also presented.

摘要

已发现一类新型的中氮茚并[1,2 - a]嘧啶酮,具有卓越的杀虫活性,能防治多种昆虫。在本通讯中,我们报告了优化计划的一部分,该计划导致发现了三氟甲吡嘧作为一种高效杀虫剂,可防治各种稻飞虱种类。我们还介绍了在发现、合成、构效关系阐明及生物活性评估方面所做的工作。

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