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.

该三环中间体2已通过八个步骤，从已知的化合物6中合成，整体产率高达20%。因此，这构成了(±)-aplykurodinone-1的高效形式合成。该合成工艺独具特色，采用一锅法、分子内异构Pauson-Khand反应（h-PKR）/去硅基化序列，迅速构建三环结构框架，为拓展h-PKR的应用范围和边界提供了宝贵的见解。