A Direct Synthesis of 3‐Acylanthranils via A One‐Pot Oxidation and Electrophilic Halogen‐Induced Annulation from 2‐Alkynylanilines

Abstract The current study features the development of a new method to convert 2‐alkynylanilines to 3‐acylanthranils which have served as a valuable retron for 2‐aminobenzaldehyde derivatives and as building blocks in conversion to other tremendously useful synthetic compounds. The method involves a carefully controlled sequential two‐step, one‐pot oxidative annulation procedure using meta ‐chloroperbenzoic acid ( m ‐CPBA) and (bis(trifluoroacetoxy)iodo)benzene (PIFA) and lithium iodide (LiI). The protocol is mild and convenient to set up while being applicable to preparing a wide array of products with good to excellent functional group tolerability and moderate to good efficiencies.