Saturated, three-dimensional scaffolds are key in modern drug discovery, and highly strained rings serve as privileged building blocks for their synthesis. Now, by tailoring the substitution patterns of 1,4-precursors, the authors suppress the competing di-π-methane rearrangement, enabling an efficient and divergent synthesis of highly strained housanes via an intramolecular [2 + 2] cycloaddition.
- Fuhao Zhang
- Julius Domack
- Frank Glorius