Late-stage synthesis of heterobifunctional molecules for PROTAC applications via ruthenium-catalysed C‒H amidation
Daniele Antermite, Stig D. Friis, Johan R. Johansson, Okky Dwichandra Putra, Lutz Ackermann, Magnus J. Johansson · 2023
Read Late-stage synthesis of heterobifunctional molecules for PROTAC applications via ruthenium-catalysed C‒H amidation by Daniele Antermite, Stig D. Friis, Johan R. Johansson, Okky Dwichandra Putra, Lutz Ackermann, Magnus J. Johansson (2023) 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-10716378.txt.
Description
Daniele Antermite and co-authors found a late-stage way to build drug-like chimera molecules in a 2023 chemistry paper. PROTACs are two-headed molecules that drag a target protein to the cell's trash system. Making them is slow, since each head and the link must be built and joined with care.
Their method uses a ruthenium catalyst to add the second head at a late step, by direct work on a carbon-hydrogen bond. It starts from parts that are easy to buy or make. A modular route like this lets chemists spin out many variants fast. That speed helps map which shapes degrade targets best.
Catalog record
| CREATOR | Daniele Antermite, Stig D. Friis, Johan R. Johansson, Okky Dwichandra Putra, Lutz Ackermann, Magnus J. Johansson |
|---|---|
| YEAR | 2023 |
| COLLECTION | PAPERS |
| FORMAT | TXT |
| FILE SIZE | 44 KB |
| VERSION | 1.0 |
| LICENSE | CC BY 4.0 |
| RIGHTS | CC BY |
| SOURCE | Europe PMC |