Air‐Assisted 2‐Oxo‐Driven Dehydrogenative α,α‐Diamination of 2‐Oxo Aldehydes to 2‐Oxo Acetamidines

Abstract

An air‐assisted, functional‐group‐driven, mild, additive‐free, three‐component synthetic approach to different 2‐oxo acetamidines from 2‐oxo aldehydes, secondary amines, and anilines was successfully developed. Mechanistically, the transformation proceeds through a highly unstable system (RCOCHN 1 N 2 ) that rearranges at room temperature and undergoes air‐assisted dehydrogenation to different 2‐oxo acetamidines.