Concise Synthesis of Indole-Fused 1,4-Diazepines through Copper(I)-Catalyzed Domino Three-Component Coupling-Cyclization-N-Arylation under Microwave Irradiation.

[摘要]：Indole-fused benzo-1,4-diazepines, e.g., I (R1 = H, Me, CF3, CO2Me; R2 = Me, All, Bn), were synthesized by copper-catalyzed domino three-component coupling-indole formation-N-arylation under microwave irradn. from a simple N-mesyl-2-ethynylaniline. This method was also applicable to the formation of heterocycle-fused 1,4-diazepines.

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