Figure 1: Reactivity of unprotected anilines with alkynes.

(a) Transition-metal-catalysed hydroamination of alkynes (a formal addition of a N–H bond across a carbon–carbon multiple bond). (b) Previous work involving transition-metal (TM)-catalysed oxidative C–H bond activation/annulation of anilines with alkynes to indole derivatives (DG, directing group; E, electron-withdrawing group). (c) In this report, reversed reactivity of anilines with alkynes in the rhodium-catalysed C–H activation/carbonylation tandem to quinoline derivatives.