使用Biotage微波合成仪进行微波条件下铜催化的N-芳基化一锅法微波合成苯达松衍生物by耐士科技

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 C–N bond formation step with tolerance toward functionalized amines.