Pd-Catalyzed direct C-H arylation of pyrrolo[1,2- a ]quinoxalines.

An efficient Pd-catalyzed direct C-H arylation of pyrrolo[1,2- a ]quinoxalines with aryl iodides is described, providing a selective route toward a series of 1-arylated and 1,3-diarylated pyrrolo[1,2- a ]quinoxalines in good yields. This method features a broad substrate scope, good functional group tolerance and gram-scale synthesis. Furthermore, the C3-thiocyanation of the arylated product is also achieved. We believe that these novel aryl-substituted pyrrolo [1,2- a ]quinoxalines will have a variety of applications in organic synthesis and medicinal chemistry.