As an important kind of organic chemical intermediates, 2- (substituted ethynyl) benzaldehyde derivatives have a high chemical reactivity due to the special conjugate system and constituted with benzene ring, substituted ethynyl group and aldehyde group. So, they have been widely applied to build up variety of the novel benzo-fused ring compounds, N-containing benzoheterocyclic compounds, O-containing benzoheterocyclic compounds, muti-membered benzoheterocyclic compounds and so on. In this paper, the application of 2- (substituted ethynyl) benzaldehyde derivatives in the field of organic synthesis are reviewed, the prospects of this compounds are also discussed. It is hoped that this review can be referred to the future application of 2- (substituted ethynyl) benzaldehyde derivatives in organic synthesis.