Palladium-Catalyzed Coupling of Polyfluorinated Arenes with Heteroarenes via C–F/C–H Activation

The first palladium-catalyzed coupling of 2-pyridyl-polyfluoroarenes and benzoxazole, thiazole, benzothiazole, benzoimidazole, oxazole or oxadiazole via a concurrent C–F/C–H activation is described. Initial mechanistic studies showed that C–F activation of perfluoroarene is likely the rate-limiting step of the catalytic cycle. This protocol provides a useful and operationally simple process to functionalized polyfluoroarenes.

本项研究描述了通过并行C-F/C-H活化首次实现2-吡啶基多氟芳烃与苯并恶唑、噻唑、苯并噻唑、苯并咪唑、恶唑或恶二唑的钯催化偶联反应。初步的机理研究表明，全氟芳烃的C-F活化可能是催化循环中的速率决定步骤。本方案提供了一种实用且操作简便的过程，用于对多氟芳烃进行官能团化。