Copper-Catalyzed Carboxamide-Directed Ortho Amination of Anilines with Alkylamines at Room Temperature
摘要:
In this report, a highly efficient method for the room temperature installation of alkyl amino motifs onto the ortho position of anilines via Cu-catalyzed carboxamide-directed amination with alkylamines is described. This method offers a practical solution for the rapid synthesis of complex arylamines from simple starting materials and enables new planning strategies for the construction of arylamine-containing pharmacophores. A single electron transfer (SET)-mediated mechanism is proposed.
The preparation and X‐ray structural characterization of aliphatic amino iodane (III) reagents has been realized. These new reagents could be used for the Cu‐catalyzed directed electrophilic amination of aryl amines.