Cobalt(III)/Chiral Carboxylic Acid‐Catalyzed Enantioselective Synthesis of Benzothiadiazine‐1‐oxides via C−H Activation

Among sulfoximine derivatives containing a chiral sulfur center, benzothiadiazine‐1‐oxides are important for applications in medicinal chemistry. Here, we report that the combination of an achiral cobalt(III) catalyst and a pseudo‐C2‐symmetric H8‐binaphthyl chiral carboxylic acid enables the asymmetric synthesis of benzothiadiazine‐1‐oxides from sulfoximines and dioxazolones via enantioselective C−H bond cleavage. With the optimized protocol, benzothiadiazine‐1‐oxides with several functional groups can be accessed with high enantioselectivity. Enantioselective synthesis of benzothiadiazine‐1‐oxides has been achieved using an achiral cobalt(III) catalyst and a pseudo‐C2‐symmetric H8‐binaphthyl chiral carboxylic acid. The hybrid catalytic system enables a rapid access to benzothiadiazine‐1‐oxides from readily available sulfoximines and dioxazolones with high enantioselectivity.