Triflumezopyrim (TFM) is a novel mesoionic pyrido[1,2-α]pyrimidinones insecticide, which acts on nicotinic acetylcholine receptors (nAChRs) and has no cross-resistance with other insecticides. Herein, we firstly developed a new continuous flow approach to synthesis 2-[3-(trifluoromethyl)phenyl]malonic acid, a key intermate of TFM, coupling with esterification, condensation, and hydrolysis. All three-step reactions were optimized and transformed into a continuous synthesis mode by three micro reaction units. Compared with the batch mode, the total reaction time and overall separation yield were improved from more than 12 h and 60 % to 18 min and 73.38 %, respectively. The solvent consumption and waste emission were significantly reduced, which also provides an eco-friendly and efficient potential tool for the development and production of mesoionic pyrido[1,2-α]pyrimidinones insecticide.

中文翻译：

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高效连续合成 2-[3-（三氟甲基）苯基]丙二酸，三氟唑吡啶的关键中间体，与酯化-缩合-水解偶联反应


Triflumezopyrim （TFM） 是一种新型中离子嘧啶[1,2-α] 嘧啶酮类杀虫剂，作用于烟碱乙酰胆碱受体 （nAChRs），与其他杀虫剂没有交叉耐药性。在此，我们首先开发了一种新的连续流方法来合成 2-[3-（三氟甲基）苯基]丙二酸，这是 TFM 的关键中介体，与酯化、缩合和水解偶联。所有三步反应均经过优化，并通过三个微量反应单元转化为连续合成模式。与间歇模式相比，总反应时间和总分离产率分别从 12 h 以上和 60 % 提高到 18 min 和 73.38 %。溶剂消耗和废物排放显着减少，这也为开发和生产中离子嘧啶[1,2-α]嘧啶酮类杀虫剂提供了一种环保高效的潜在工具。