Visible Light‐Driven <i>E</i>‐Selective Semihydrogenation of Alkynes and Their Application in the Treatment of Glioblastoma Multiforme

A visible light‐driven E ‐selective semihydrogenation scheme of alkyne compounds is developed for designing and synthesizing glioblastoma multiforme inhibitors. Herein, room‐temperature semihydrogenation reactions of various alkyne compounds are successfully achieved under the irradiation of white light. The representative reaction mechanism is decoded through theoretical calculations and deuteration experiments, revealing the critical roles played by [Ir(Cp‐Me 5 )Cl 2 ] 2 , PdCl 2 , DPPE and TEOA as photosensitizer, catalyst, ligand, and electron donor, respectively. This method exhibits excellent E ‐selectivity and broad functional group compatibility and demonstrates its practical value by producing pinosylvin and its derivatives with strong inhibitory effects on U87 cells.