Abstract One-pot synthetic strategy has been developed to access isoquinolines and its analogs via Cu-mediated tandem cross-coupling and cyclization in good yields under mild reaction conditions. A mixture of suitably substituted α-bromoaldehyde, terminal alkyne, and aq NH 3 in CuI/1, 10-phenanathroline catalytic system afforded the 3-substituted isoquinoline regio-selectively in good to excellent yields.
