Functionalizations of Aryl C-H Bonds in 2-Arylpyridines via Sequential Borylation and Copper Catalysis

Selective functionalizations of aryl C-H bonds in 2-arylpyridines have been developed via sequential borylation and aerobic oxidative copper catalysis, and the corresponding aryl halides, sulfones, azides and arylamines were obtained in good yields. The protocol uses cheap and readily available boron tribromide (BBr3) as the borylating reagent, and in-organic salts (potassium iodide, ammonium bromide, sodium alkylsulfinates, sodium azide) as the functional group sources. This method makes functionalizations of aryl C-H bonds easy.