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已由已知化合物6经八步反应合成，总收率达20%。据此，本研究完成了(±)-aplykurodinone-1的高效形式合成。该合成路线采用独特的一锅法分子内杂原子Pauson-Khand反应（h-PKR）/脱硅基串联序列，快速构建三环骨架，为拓展杂原子Pauson-Khand反应的适用范围与边界提供了重要参考价值。