Copper(i)-catalyzed tandem C–N coupling/condensation cyclization for the synthesis of benzothiadiazine 1-oxides

Abstract

A highly efficient and straightforward strategy for the synthesis of benzothiadiazine 1-oxides has been developed, involving a copper(I)-catalyzed tandem C–N coupling/condensation cyclization of ortho-haloaryl organyl NH-sulfoximines and aromatic/aliphatic amidines. This protocol exhibits several notable advantages, including the absence of a requirement for an additional nitrogen source, a broad substrate scope, mild reaction conditions, and significant potential for application in the industrial production of benzothiadiazine 1-oxides.