Stainless-steel-initiated acylation of quinoxalin-2(1H)-ones with aldehydes under mechanochemical conditions

Abstract

Utilizing direct mechanocatalytical conditions, we have developed a C–H acylation of quinoline-2(1H)-one initiated by stainless-steel milling balls. A wide range of functional groups are bearable, affording the desired products in excellent yields. Noteworthy is the short reaction period (30 min) and no requirement for solvent. The late-stage functionalization of pharmaceutical-related molecules illustrates its potential application in drug development. Gram-scale synthesis further demonstrates the scalability and sustainability of this method.