Gold-catalyzed oxidative coupling of alkynes was developed as an efficient approach for the synthesis of challenging cyclic conjugated diynes (CCD). Compared with the classic copper-promoted oxidative coupling reaction of alkynes, this gold-catalyzed process exhibited a faster reaction rate due to rapid reductive elimination from the Au(III) intermediate. This unique reactivity thus allowed a challenging diyne macrocyclization to take place with high efficiency. Condition screening revealed an [(n-Bu)₄N]⁺[Cl-Au-Cl]⁻ salt as the optimal pre-catalyst. Macrocycles with ring size between 13 and 28 atoms were prepared in moderate to good yields, which highlighted the broad substrate scope of this new strategy. Furthermore, the synthetic utilities of the CCDs for copper-free click chemistry have been demonstrated, showcasing the potential application of this strategy in biological systems.

炔烃的金催化氧化偶联被开发为合成具有挑战性的环状共轭二炔（CCD）的有效方法。与经典的炔烃铜促进的氧化偶联反应相比，由于金（III）中间体的快速还原消除，这种金催化的方法显示出更快的反应速率。因此，这种独特的反应性使得高效的挑战性二炔大环化发生。条件筛选显示[[（n -Bu）₄ N] ⁺ [Cl-Au-Cl] ^-盐作为最佳的前催化剂。以中等至良好的产率制备了具有13至28个原子的环大小的大环化合物，这突出了该新策略的广泛底物范围。此外，已经证明了用于无铜点击化学的CCD的合成效用，表明了该策略在生物系统中的潜在应用。