A Metal‐Free Route to 2‐Aminooxazoles by Taking Advantage of the Unique Ring Opening of Benzoxazoles and Oxadiazoles with Secondary Amines

Toss an amine into the ring: A new metal-free protocol for the amination of oxazoles has been developed by using iodobenzene diacetate to couple various oxazoles with amines (see scheme). The reaction proceeds through a ring-opening and subsequent ring-closing pathway. The optimal conditions are very mild and the substrate scope is broad, producing a range of 2-aminooxazoles, an important pharmacophore with high bioactivity.