An efficient I ₂ -catalyzed cascade coupling protocol was developed for the synthesis of pyrrolo[1,2- a ]quinoxaline and imidazo[1,5- a ]quinoxaline derivatives via sp ³ and sp ² C–H cross-dehydrogenative coupling.

An efficient and convenient one-pot domino reaction for the direct synthesis of pyrrolo[1,2-a]quinoxalines has been developed. This approach utilizes an imine formation reaction, S_EAr reaction and cleavage of C–C bonds catalyzed by a Brønsted acid. β-Diketones and β-keto esters are both well tolerated to give the corresponding products in moderate to excellent yields.

A transition metal-free process for the regioselective synthesis of pyrrolo[1,2-a]quinoxalines under mild conditions in one-pot is described. The reaction afforded a variety of products in good to excellent yields. Indolo[1,2-a]quinoxalines were also synthesized from indole-2-carboxamides under the same conditions.