Mesoionic pyrido[1,2-a]pyrimidinones: Discovery of triflumezopyrim as a potent hopper insecticide¹

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• 作者：Wenming Zhang^a ; ^{wenming.zhang@dupont.com} ; Caleb W. Holyoke Jr.^a ; Thomas F. Pahutski^a ; George P. Lahm^a ; James D. Barry^a ; Daniel Cordova^a ; Robert M. Leighty^a ; Vineet Singh^b ; Daniel R. Vicent^a ; My-Hanh T. Tong^a ; Kenneth A. Hughes^a ; Stephen F. McCann^a ; Yewande T. Henry^a ; Ming Xu^a ; Twyla A. Briddell^a
• 关键词：Mesoionic ; Pyrido[1 ; 2-a]pyrimidinone ; Insecticide ; Triflumezopyrim ; Acetylcholine receptor ; Inhibitor
• 刊名：Bioorganic & Medicinal Chemistry Letters
• 出版年：2017
• 出版时间：1 January 2017
• 年：2017
• 卷：27
• 期：1
• 页码：16-20
• 全文大小：789 K
• 卷排序：27

文摘

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.