One-Pot Synthesis of Benzene and Pyridine Derivatives via Copper-Catalyzed Coupling Reactions

A highly efficient one-pot synthesis of polysubstituted pyridine has been achieved through copper-catalyzed oxidative sp(3) C-H coupling of acetophenones with toluene derivatives. Besides, the polysubstituted benzene was obtained through copper-catalyzed coupling of acetophenones. Both of the reactions exhibited a good functional group tolerance to produce a 2,4,6-triphenylpyridine or 1,3,5-triarylbenzene in high yields. Compared with previous methods, these transformations allow a highly flexible and efficient preparation of substituted pyridines and benzenes.