Cover Picture: Remote C(sp3)−H Acylation of Amides and Cascade Cyclization via N‐Heterocyclic Carbene Organocatalysis (Angew. Chem. Int. Ed. 15/2022)

Abstract

An NHC-organocatalyzed remote C(sp3)−H acylation of amides is developed based on a 1,5-hydrogen atom transfer strategy. As reported in the Research Article by Jun-Long Li et al. (e202116629), over 120 functionalized δ-amino ketones and isoquinolinones were synthesized in up to 99 % yield under mild conditions. Mechanistic investigations, including control reactions, KIE experiments, and computational studies, shed light on the organocatalytic radical reaction mechanism.