吗啉中钯催化的Suzuki-Miyaura反应研究

Morpholine as an Efficient Ligand and Reaction Medium for Phosphane-Free Palladium-Catalyzed Suzuki-Miyaura Reaction

以吗啉为配体和反应介质下,介绍了钯催化、无膦配体的Suzuki-Miyaura反应体系。在n(ArX)=1.00mmol,n(ArB(OH)_2)=1.00mmol,x(Pd(OAc)_2)=0.01mmol,n(K_2CO_3)=2.00mmol,v(吗啉)=4mL的优化条件下,芳基碘化物、芳基溴化物能够与苯硼酸高产率生成Suzuki-Miyaura交叉偶联产物,具有反应条件温和、操作简单、无需膦配体的特点。

An efficient protocol has been developed for the phosphane-free Pd（OAc） 2-catalyzed Suzuki- Miyaura reaction in morpholine. Under the optimized reaction conditions （ 1.00 mmol organic halide, 1.00 mmol boronic acid,0.01 mmol Pd（ OAc）2,2.00 mmol K2CO3 and 4 mL morpholine at 80℃ for 5 h）, aryl iodides and bromides, coupled with organoboronic acids, smoothly afford the cross-coupling products in good to excellent yields.