Copper-Catalyzed Intramolecular N–S Bond Formation by Oxidative Dehydrogenative Cyclization

Copper-catalyzed synthesis of benzo­[d]­isothiazol-3­(2H)-ones and N-acyl-benzothiazetidine by intramolecular dehydrogenative cyclization is described. In this reaction, a new nitrogen–sulfur (N–S) bond is formed by N–H/S–H coupling. The present reaction has high functional group tolerance and gives products in gram scale. This method promotes double cyclization, allowing for synthesis of a drug intermediate.本文报道了一种通过分子内脱氢环化反应实现铜催化合成苯并[d]异噻唑-3(2H)-酮与N-酰基苯并硫杂环丁烷的方法。该反应通过N–H/S–H偶联构筑了全新的氮-硫（N–S）键。本反应具有优异的官能团耐受性，可实现克级规模的产物制备。该方法可促进双重环化过程，能够用于合成药物中间体。