Jia-Jun Qiao, Yi-Ming Ma, Zhi-Tao He
Propargylic substitution is a basic transformation model in organic synthesis, which requires the adoption of alkyne substrates bearing a vicinal leaving group. Recently, the exploration of remote-leaving-group-promoted propargylic substitution pioneered by Fang, He and Xu, has gained much attention and provided new possibilities for this classical area. With this design, a series of related studies have been reported and enabled the enantioselective construction of diverse privileged skeletons. This review article provides a detailed summary of the origin, development, mechanisms, limitations and future directions of this nonclassical propargylation model.