Ketemines represent an interesting class of organic intermediates that has undergone a regrowth as a consequence of recent extensions of copper catalyzed azide alkyne cycloaddition (Cu- AAC) to other synthetic fields. This review summarizes the most recent generation methods of ketimines from CuAAC reaction, highlighting chemical properties focused on the synthesis of cyclic compounds, among others, affording a general outlook towards the development of new biologically active compounds.