Abstract
Highly substituted isoquinolines are an important class of heterocycles and are found in many naturally occurring compounds, and they are broadly used industrially in dyes, paints, OLEDs, and drugs synthesis. So the synthesis of isoquinolines is an important issue recently. Herein, We describe a convenient and highly regioselective synthesis of substituted isoquinoline derivatives from C－N and C－C crosscoupling between hydrazones and alkynes using a catalytic amount of [RhCp*Cl2]2, acetic acid (AcOH) and silver oxide (Ag2O) in the presence of methanol, a process that involves ortho-C－H activation of hydrazones and alkynes, and a likely mechanism has been suggested.