Reductive Rearrangement of Substituted Quinolines to 2,3-Disubstituted Indoles Enabled by Water Activation

Abstract

Herein, we report a selective reductive rearrangement of substituted quinolines into indoles — a privileged structural motif widely found in natural products and bioactive molecules. This quinoline skeletal editing is accomplished through water activation mediated by photocatalytically generated phosphine radical cations. The developed protocol provides a robust and broadly applicable approach for synthesizing diverse indole derivatives from readily available quinoline substrates.