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… Click to show full 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.
               
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