1H-Indole-3-carboxaldehyde and its derivatives have represented the key intermediates for the preparation of biologically active compounds as well indole alkaloids. Also they are important precursors for the synthesis of divers heterocyclic derivatives because their carbonyl groups facilely undergo C–C and C–N coupling reactions and reductions. This review highlights the recent advances in 1H-indole-3-carboxaldhyde chemistry via discussing different synthetic procedures developed for the preparation of its derivatives, as well sheds the light on the most common reactions of 1H-indole-3-carboxaldhyde derivatives and exploitation of these derivatives as the blocks of many biologically active compounds.