Copper-Mediated ortho-C-H Amination Using DMF as the Amine Source.

Abstract

We report herein a copper-mediated ortho-C-H amination of anilines using oxalamide as the directing group and DMF as the amination reagent. This protocol tolerates various functional groups and shows good heterocyclic compatibility. Late-stage dimethylamination of drugs demonstrated the synthetic practicality of the protocol. Mechanistic experiments indicate that a radical pathway may be involved in the reaction.