An Efficient Domino Synthesis of Quinoxalin-2(1H)-ones via an SNAr/Coupling/Demesylation Reaction Catalyzed by Copper(I) as Key Step

An efficient copper-catalyzed method for the synthesis of quinoxalin-2(1H)-ones derivatives via domino SNAr/coupling/demesylation reaction of N-(2-halophenyl)methylsulfonamides with 2-halo amides has been developed. Various quinoxalinones with diversity at three positions on their scaffold have been obained, and the method is valuable for the construction of this kind of molecules with biological and pharmaceutical activities.