Auto‐Oxidation‐Induced Construction of Isatins from Glycine Derivatives

Abstract

An oxygenation approach to isatins via an autooxidation/intramolecular annulation tandem reaction of glycine derivatives is described. This transformation provides a metal-free protocol for the preparation of isatin derivatives, which are important structural motifs widely found in organic molecules with various functions and privileged units for the synthesis of complex heterocycles. The reaction proceeds smoothly under mild reaction conditions and requires only Brønsted acid and oxygen. . Auto-oxidation of various alkyl 2-(methyl(p-tolyl)amino)acetates a,b .Scheme 3. Auto-oxidation of methyl 2-(methyl(aryl)amino)acetate a,b .Scheme 4. Auto-oxidation of methyl 2-((4-methoxyphenyl)(alkyl)amino)acetate a,b .