Facile synthesis of 3-(aminomethyl)isoquinolines by copper-catalysed domino four-component coupling and cyclisation.

Copper(i)-catalysed domino four-component coupling-cyclisation using 2-ethynylbenzaldehydes, paraformaldehyde, secondary amine, and t-BuNH(2) in DMF leads to direct and efficient formation of 3-(aminomethyl)isoquinolines in good to high yields.