Copper-catalyzed N-arylation of isatins employing aryl(TMP)-iodonium salts

Abstract

This work presents a general one-pot methodology for N-arylation of isatin functionalities employing aryl(2,4,6-trimethoxyphenyl)iodonium salts. The developed Cu-catalysed protocol works under mild conditions and is operationally straightforward. This synthetic approach demonstrates broad substrate scope, tolerating a wide range of electronically and sterically diverse aryl groups, thereby enabling access to a variety of N-arylated isatin products. Furthermore, two examples of post-synthetic modification highlight the utilization of the synthetic scaffolds.