Rh(III)‐Catalyzed Sequential ortho‐C‐H Bond Annulation and Desulfonylation of 3‐Aryl‐2H‐benzothiadiazine‐1,1‐dioxides: Access to 1‐Aminoisoquinolines

An efficient Rh(III)‐catalyzed C−H functionalization of 3‐aryl‐2H‐benzo[e][1,2,4]thiadiazine‐1,1‐dioxides with diaryl and dialkyl alkynes has been developed for the first time to the synthesis of 1‐aminoisoquinoline derivatives in a single step. This method involves through the formation of one C−C bond and one C−N bond followed by desulfonylation to generate a novel series of isoquinolines in good to excellent yields. This is a direct method to produce pharmaceutically more relevant scaffolds with a high functional diversity.