A unified platform for the rapid assembly of glutarimides for Cereblon E3 ligase modulatory drugs
David M Whalley, Olivier Lorthioir, Niall A Anderson, Erin Braybrooke, Susannah C Coote, Sylvain Demanze, Holly L Douglas, Okky Dwichandra Putra, Katie Proctor, Yuanyuan Si, Sam Staniland, Stephen Stokes, Alfie Woodhouse · 2026
Read A unified platform for the rapid assembly of glutarimides for Cereblon E3 ligase modulatory drugs by David M Whalley, Olivier Lorthioir, Niall A Anderson, Erin Braybrooke, Susannah C Coote, Sylvain Demanze, Holly L Douglas, Okky Dwichandra Putra, Katie Proctor, Yuanyuan Si, Sam Staniland, Stephen Stokes, Alfie Woodhouse (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/PMC13439528.txt.
Description
David M Whalley and co-authors unveil a fast, single route to glutarimide building blocks prized in protein-degrader drugs, reporting in 2026. Glutarimides anchor medicines that hijack cereblon, a cell protein that tags other proteins for disposal. Drugs from thalidomide kin to newer degraders rely on the motif, yet older syntheses took many steps and slowed testing of new variants. Their platform starts from common nitrogen ring compounds and runs three steps in sequence.
A phosphine-catalysed bond formation, a metal-free radical addition, and an acid-driven ring closing deliver varied glutarimides with high selectivity. The route tolerates many chemical groups and scales from grams to rapid parallel batches. With it, the team built cereblon binder libraries, control analogues, and late-stage tweaks of active molecules. The authors pitch the platform as a way to speed degrader discovery.
Catalog record
| CREATOR | David M Whalley, Olivier Lorthioir, Niall A Anderson, Erin Braybrooke, Susannah C Coote, Sylvain Demanze, Holly L Douglas, Okky Dwichandra Putra, Katie Proctor, Yuanyuan Si, Sam Staniland, Stephen Stokes, Alfie Woodhouse |
|---|---|
| YEAR | 2026 |
| COLLECTION | PAPERS |
| FORMAT | TXT |
| FILE SIZE | 40411 |
| LICENSE | https://creativecommons.org/licenses/by/4.0 |
| RIGHTS | CC BY |
| SOURCE | Europe PMC |