Total Synthesis of (±)-Dhilirolide U
We report the first total synthesis of (±)-dhilirolide U, a highly oxidized meroterpenoid featuring a densely functionalized 6/6/6/5/5-pentacyclic skeleton. Central to the strategy are a Mn<sup>III</sup>-mediated cyclization sequence and a Payne-type rearrangement cascade, which together forge a bicyclo[3.2.1]octane fused to a γ-lactone─the defining motif of the dhilirolide natural product family. Both transformations proceed in high yields and with excellent diastereocontrol. Intramolecular Ni-catalyzed conjugate addition was leveraged to install the vicinal quaternary carbon centers. This transformation set the stage for construction of the tetrahydroisochromenone subunit and completion of (±)-dhilirolide U. The reported route to the highly decorated bicyclo[3.2.1]octane provides a blueprint to access the diverse family that are the complex dhilirolide meroterpenoids.
Authors
- Marlene Fadel (ORCID: https://orcid.org/0000-0002-2790-710X)
- Oscar García González
- Henrik R. Wilke (ORCID: https://orcid.org/0000-0002-1954-3123)
- V. S. Avramenko
- Kacper J. Patej (ORCID: https://orcid.org/0009-0000-4000-1006)
- Nima Nasiri (ORCID: https://orcid.org/0000-0002-4719-7811)
- Rüveyda Bal
- Tobias K Jenny
- Jameel Ahmad
- Matteo C Amberg
- Jan P Prohaska
- Jonathan Kastner
- Erick M Carreira
Institutions
- ETH Zurich (CH)
Publication Details
- Journal
- Journal of the American Chemical Society
- Published
- 2026-02-09
- DOI
- https://doi.org/10.1021/jacs.5c22734
- Citations
- 1
- Primary Topic
- Marine Sponges and Natural Products
- Type
- article
- Field-Weighted Citation Impact
- 27.96