Organocatalytic Enantioselective Synthesis of C-N Axially Chiral N-Arylindole Amino Esters via Oxidative Esterification with Dynamic Kinetic Resolution.

A highly efficient N-heterocyclic carbene (NHC)-catalyzed dynamic kinetic resolution strategy has been developed for the selective oxidative esterification of N-sulfonamide aminoaldehydes. With a catalyst loading as low as 3 mol %, a broad range of structurally diverse N-arylindole amino esters featuring a C-N chiral axis were synthesized in excellent yields and enantioselectivities. The reaction exhibits broad substrate scope and has been successfully performed on a gram scale, demonstrating its high efficiency and practical utility.