Abstract

Polycyclic N-heterocycles are very important scaffolds in biomedicinal chemistry and materials science. Intramolecular alkyne hy-droamination is a powerful method for the construction of N-heterocycles. In the last two decades, copper-catalyzed domino reac-tions based on intramolecular alkyne hydroamination has emerged as a robust strategy for assembling various polycyclic N-heterocycles. Great progress has been achieved in this area. This short review covers the advances made in copper-catalyzed domino synthesis of polycyclic N-heterocycles based on this strategy from 2008 to 2023, and will hopefully serve as an inspiration towards the exploration of new copper-catalyzed versions of the transformation. The domino transformations are introduced and discussed from five aspects according to the different key processes involved in these reactions.