Quinoline-Fused Lactones via Tandem Oxidation Cyclization: Metal-Free sp³ C–H Functionalization

Abstract

A unique lactonization of 2-methyl-3-acyl-4-phenylquinolines using PhIO as the oxidant and selectfluor as an additive is reported. The reaction occurs under ambient conditions through tandem oxidation and cyclization of sp3 C–H bonds under metal-free conditions. The heterocycle-fused lactones are obtained in moderate to good yield.