Acynonapyr, discovered by Nippon Soda Co., Ltd., is a novel acaricide with N-pyridyloxy azabicycle as a unique core structure. Acynonapyr exhibits high activity against the spider mite species in the genera Tetranychus and Panonychus, with good efficacy at all life stages. Early in this research, cyclic amines substituted with (hetero)aryl(oxy) moieties were designed as target molecules and diversely synthesized, and 4-[4-(trifluoromethyl)phenoxy]-1-[5-(trifluoromethyl)-2-pyridyl]piperidine was found to show weak acaricidal activity. The structural optimization of this acaricidal active piperidine as the first lead compound led to the discovery of acynonapyr. In this report, our research process that led to the discovery of acynonapyr is described.

Acynonapyr是日本曹达株式会社发现的一种以N-吡啶氧基氮杂双环为独特核心结构的新型杀螨剂。Acynonapyr 对叶螨属和全爪螨属的叶螨表现出高活性，在所有生命阶段均具有良好的功效。在这项研究的早期，被（杂）芳基（氧基）部分取代的环胺被设计为目标分子并进行了多种合成，4-[4-（三氟甲基）苯氧基]-1-[5-（三氟甲基）-2-吡啶基]发现哌啶显示出弱的杀螨活性。这种杀螨活性哌啶作为第一个先导化合物的结构优化导致了 acynonapyr 的发现。在本报告中，描述了我们发现 acynonapyr 的研究过程。