Transition-Metal-Free Synthesis of 7-Aminocoumarins from 7-Hydroxycoumarins Using Multifunctional Reagent

Abstract

We have successfully synthesized N-substituted 7-aminocoumarins by reacting 7-hydroxycoumarins with amines using 5,6-dichloro-2,3-dicyanopyrazine, a readily available multifunctional reagent. This reagent effectively brings both coupling partners into close proximity, facilitating dehydrative C─N coupling reactions under mild, metal-free conditions. Our approach demonstrates a broad substrate scope and enables gram-scale production. © 2025 Wiley-VCH GmbH.