A microwave-assisted, sequential, one-pot protocol has been developed for the synthesis of a variety of benzothiadiazin-3-one-1,1-dioxides. This protocol utilizes a copper catalyzed N-arylation of a-bromobenzenesulfonamides with a number of amines to generate the corresponding 2 aminobenzenesulfonamides,which undergo cyclization to the desired sultams using carbonyl diimidazole (CDI). A range ofconditions was evaluated for the key CN bond formation step with tolerance toward functionalized amines. Biotage 微波合成儀 Initiator+ Biotage 微波合成儀 Initiator Biotage 微波合成儀 Initiator+ Robot 8 Biotage 微波合成儀 Initiator+ Robot 60