Copper-Catalyzed Tandem Synthesis of N-Fused Isoquinolines

Significance

This work provides a facile and direct synthesis of substituted indolo- and pyrrolo[2,1-a]isoquinolines from ortho-halogenated aromatic alkynes and indole or pyrrole deriva-tives, respectively. Copper salts such as CuI or Cu(OAc)₂ serve as catalyst with (hydroxymethyl)benzotriazole as ligand, affording the condensed aromatic products in good yields and excellent regioselectivity.