Synthesis of 3,4-Functionalized Benzothiazines through C-H Activation

A method for the synthesis of a wide range of 1,2-benzothiazines bearing pyridyl, amide, sulfonamide, alkenyl, as well as aryl groups in 3,4-position has been developed using transition metal-catalyzed C-H activation reactions of pyridylbenzothiazines with dioxazolones, tosyl azide, alkenes, alkynes, and diaryliodonium salts. The present reaction provides an efficient method for the synthesis of a variety of 3,4-functionalized benzothiazines from readily available starting materials and benefits a broad substrate scope, high functional group tolerance, and good regioselectivity.

Automated summary

A method for the synthesis of a wide range of 1,2-benzothiazines bearing various functional groups has been developed using transition metal-catalyzed C-H activation reactions, providing efficient synthesis from readily available starting materials with broad substrate scope and good regioselectivity.