Abstract A novel synthetic route for arylated 1, 4-benzothiazine derivatives has been developed. This method utilizes a key intramolecular nucleophilic aromatic substitution step of the corresponding (Z)-β-(2-fluorobenzenesulfonyl) vinylamine intermediate to construct the benzothiazine ring. A wide range of aryl and heteroaryl substituent groups can be installed from commercial boronic acids. Both mono-and diarylated products have been ...