Abstract

AbstractA metal‐catalyzed regioselective approach towards the synthesis of 1‐aminoisoquinolines and/or 1‐aminoisindolines through aminative domino cyclization of 2‐alkynylbenzonitriles with secondary amines has been developed under solvent‐free conditions. It was found that the regioselectivity of the reaction was greatly influenced by the choice of the metal catalyst. Copper‐based catalysts favored 6‐endo‐dig cyclization leading to 1‐aminoisoquinolines, whereas other catalysts such as triflates of Zn, Ag, Bi, Sc and Yb favored the formation of 1‐aminoisoindolines through 5‐exo‐dig cyclization.

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