Ligand- and Additive-Free CuCl2-Catalyzed para-C-H Alkylation of Aniline Derivatives via Carbene Insertion

Transition metal-catalyzed C-H insertion reaction is a straightforward strategy to realize the direct functionalization of electric-rich (hetero)arenes. The known methods generally require metal catalysts chelating with well-defined ligands and the use of additives; a simple and practical catalytic system is still needed. We herein report a ligand- and additive-free, CuCl2-catalyzed highly selective para-C-H carbene insertion of aniline derivatives using alpha-aryl-alpha-diazo esters. A diverse array of 1,1-diarylacetates were obtained in high yields with excellent chemo- and regioselectivity.

Automated summary

The study presents a ligand- and additive-free CuCl2-catalyzed highly selective para-C-H carbene insertion reaction, which can produce a variety of 1,1-diarylacetates with high yields and excellent selectivity.