Microwave-assisted sequential one-pot protocol to benzothiadiazin-3-one-1,1-dioxides via a copper-catalyzed N-arylation strategy

作者：Rolfe Alan; Hanson Paul R^*

来源：Tetrahedron Letters, 2009, 50(50): 6935-6937.

DOI：10.1016/j.tetlet.2009.09.090

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 alpha-bromo-benzenesulfonamides with a number of amines to generate the corresponding 2-aminobenzenesulfonamides, which undergo cyclization to the desired sultams using carbonyl diimidazole (M). A range of conditions was evaluated for the key C-N bond formation step with tolerance toward functionalized amines.

• 出版日期2009-12-16