Aerobic Oxidative Cascade Thiolation and Cyclization to Construct Indole-Fused Isoquinolin-6(5H)-one Derivatives in EtOH

A practical method to construct sulfenylated indole-fused isoquinolin-6(5H)-one derivatives has been developed. Using eco-friendly ethanol as the solvent and air as the oxidant, this reaction could be compatible with sensitive molecular framework. The utility of the product was well illustrated by further transformations. Moreover, the reaction mechanism was investigated by control experiments.