A Chemo-Selective [4 + 2] Annulation for the Construction of 3,1-Benzothiazine and Tetrahydroquinazoline Functionalized Sulfonyl Fluoride Pharmacophores

A chemoselective [4 + 2] annulation protocol employing 2-aminostyrylsulfonyl fluoride and isothiocyanates was established, enabling selective access to two distinct classes of 3,1-benzothiazine- and tetrahydroquinazoline-functionalized sulfonyl fluorides. This method provides a novel approach for constructing highly functionalized sulfonyl fluoride pharmacophores that hold significant potential in the fields of medicinal chemistry, chemical biology, and drug discovery.