溴虫氟苯双酰胺的温和双线型合成路线

溴虫氟苯双酰胺(Broflanilide) 是由日本三井农业化学公司和巴斯夫联合开发的作用于γ-氨基丁酸(GABA)受体的双酰胺类杀虫剂, 高效、低毒且与传统杀虫剂无交互抗性等一系列优点使其得到了迅速的推广和应用, 如何更好地实现溴虫氟苯双酰胺的工业化生产, 开发出反应条件温和且收率较优的合成路线成为了当下农药工作者关注的重心。结合文献调研结果和经典的有机反应, 设计了溴虫氟苯双酰胺的合成路线, 通过一系列实验探究, 发现通过调控官能团的取代顺序, 控制空间位阻效应对反应活性的影响, 在常规无机盐碘化钾(KI) 的催化作用下, 便可温和且较优产率(38%) 收获目标产物, 避免了强碱低温或者高沸点溶剂等苛刻条件的使用。

A Mild Bilinear Synthesis Route of Broflanilide

The Diamide insecticide Broflanilide acting on GABA receptor, which were developed by Mitsui Agricultural Chemical Company and BASF Corporation. A series of advantages led to their rapid promotion and application, such as high efficiency, low toxicity, and no cross resistance with traditional insecticides. Develop the synthesis route with warm reaction conditions and high yieldto achieve the industrial production of Broflanilide by better route which is the focus of current pesticide workers. Based on the literature research results and the classic organic reactions, the synthesis route for Broflanilide were designed. Through a series of experiments, it is found that the target product can be gently and efficiently (38%) harvested under the catalysis of conventional inorganic salt potassium iodide (KI) by regulating the substitution order of functional groups and controlling the effect of steric hindrance on reactivity, which avoids the use of harsh conditions such as strong alkali low temperature or high boiling point solvent.