One-pot C2-arylation and C4-acetoxylation of tryptophan derivatives via palladium-catalyzed tandem C–H activation

Abstract

Herein, we disclosed a dual-functionalization of tryptophan derivatives at the C2 and C4 positions of the indole ring through a palladium-catalyzed cascade C–H activation. This step-economical protocol features operational simplicity under mild conditions, achieving concurrent aryl and acetoxy group installation in one pot, making it a straightforward approach to efficiently synthesize highly decorated tryptophan derivatives. Furthermore, gram-scale synthesis and further transformation were also feasible, demonstrating the robustness of this method.