Formal Synthesis of (±)-Aplykurodinone‑1 through a Hetero-Pauson–Khand Cycloaddition Approach

The tricyclic intermediate 2 has been synthesized in eight steps from known compound 6 in 20% overall yield. As such, this constitutes a highly efficient formal synthesis of (±)-aplykurodinone-1. This synthesis features a unique, one-pot, intramolecular hetero-Pauson-Khand reaction (h-PKR)/desilylation sequence to expeditiously construct the tricyclic framework, providing valuable insights for expanding the scope and boundaries of h-PKR.三环中间体2以已知化合物6为起始原料，经八步反应合成得到，总产率为20%。据此，该工作实现了(±)-aplykurodinone-1的高效形式合成。该合成路线采用了独特的一锅法分子内杂原子Pauson-Khand反应（hetero-Pauson-Khand reaction, h-PKR）/脱硅基化串联过程，可快速构建三环骨架，为拓展h-PKR的适用范围与边界提供了有价值的研究思路。