A Scalable Stereoselective Synthesis of Polysubstituted Housanes
Valentin V. Veselinov, Ayan Dasgupta, Andreas Pielmeier, Adrián López-Francés, Hafdís Haraldsdóttir, Kirsten E. Christensen, Edward A. Anderson · 2026
Read A Scalable Stereoselective Synthesis of Polysubstituted Housanes by Valentin V. Veselinov, Ayan Dasgupta, Andreas Pielmeier, Adrián López-Francés, Hafdís Haraldsdóttir, Kirsten E. Christensen, Edward A. Anderson (2026) in the Tower of Babel, a free online library of public-domain works preserved in clean, searchable text. No sign-up. The full text is served as a plain-text file at a predictable URL, where text is present: https://antarctic-labs.com/tower-of-babel/pmc-13270642.txt.
Description
Valentin V Veselinov and co-authors present in 2026 a scalable way to decorate housanes, tiny cage-like hydrocarbons proposed as stand-ins for benzene rings in drug design. Housanes drew little attention because adding groups late, and in the right places, was hard. Their method uses a directing group to guide metalation first at the bridgehead, then along the fused three-membered ring.
The sequence gave two- and three-substituted housanes with excellent control of position and shape. Crystal structures and calculations checked how well the products mimic ortho-substituted benzene geometry. A boron-mediated rearrangement turned one housane into a crowded cyclopentane boronic ester, and a mirror-selective variant gave a single handed form. The work opens housanes to the late-stage variety that drug chemists expect.
Catalog record
| CREATOR | Valentin V. Veselinov, Ayan Dasgupta, Andreas Pielmeier, Adrián López-Francés, Hafdís Haraldsdóttir, Kirsten E. Christensen, Edward A. Anderson |
|---|---|
| YEAR | 2026 |
| COLLECTION | PAPERS |
| FORMAT | TXT |
| FILE SIZE | 14 KB |
| VERSION | 1.0 |
| LICENSE | CC BY 4.0 |
| RIGHTS | CC BY |
| SOURCE | Europe PMC |