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Synthesis and biological activity of a novel fungicide pyraziflumid

机译:新型杀菌剂吡嗪氟胺的合成及生物活性

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摘要

Pyraziflumid was discovered as a novel SDHI fungicide chemically characterized by the 3-(trifluoromethyl)pyrazine-2-carboxamide group. This chemical series showed particularly high fungicidal activities against a broad spectrum of plant diseases in the case of N-(biphenyl-2-yl) as well as N-(1,1,3-trimethylindan-4-yl)carboxamides. Various N-(biphenyl-2-yl)pyrazine-2-carboxamides were synthesized, and their structure–activity relationships were studied. The optimization of the fungicidal performance of the series finally led to the identification of pyraziflumid, which could control a wide range of plant diseases. In this report, details of the structure–activity relationships from the lead compound to pyraziflumid are described.
机译:吡吡氟胺是一种新型的SDHI杀菌剂,其化学特征是3-(三氟甲基)吡嗪-2-羧酰胺基团。在N-(联苯-2-基)以及N-(1,1,3-三甲基茚满-4-基)羧酰胺的情况下,该化学系列显示出对多种植物疾病的极高杀真菌活性。合成了各种N-(联苯-2-基)吡嗪-2-羧酰胺,研究了它们的结构-活性关系。该系列产品杀菌性能的优化最终导致了吡唑氟虫胺的鉴定,该吡嗪氟虫胺可以控制多种植物病害。在本报告中,详细介绍了从铅化合物到吡唑氟虫酰胺的构效关系。

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