Novel library synthesis of 3,4-disubstituted pyridin-2(1H)-ones via cleavage of pyridine-2-oxy-7-azabenzotriazole ethers under ionic hydrogenation conditions at room temperature
oleh: Romain Pierre, Anne Brethon, Sylvain A. Jacques, Aurélie Blond, Sandrine Chambon, Sandrine Talano, Catherine Raffin, Branislav Musicki, Claire Bouix-Peter, Loic Tomas, Gilles Ouvry, Rémy Morgentin, Laurent F. Hennequin, Craig S. Harris
| Format: | Article |
|---|---|
| Diterbitkan: | Beilstein-Institut 2021-01-01 |
Deskripsi
In our hands, efficient access to the 4-amino-3-carboxamide disubstituted pyridine-2(1H)-one kinase hinge-binder motif proved to be more challenging than anticipated requiring a significant investment in route scouting and optimization. This full paper focuses on the synthesis issues that we encountered during our route exploration and the original solutions we found that helped us to identify two optimized library-style processes to prepare our large kinase inhibitor library.