Details

Autor(en) / Beteiligte

• Kim, Jungchul
• Itoh, Tetsuji
• Xu, Feng
• Dance, Zachary E. X
• Waldman, Jacob H
• Wallace, Debra J
• Wu, Feiyue
• Kats-Kagan, Roman
• Ekkati, Anil R
• Brunskill, Andrew P. J
• Peng, Feng
• Fier, Patrick S
• Obligacion, Jennifer V
• Sherry, Benjamin D
• Liu, Zhijian
• Emerson, Khateeta M
• Fine, Adam J
• Jenks, Anna V
• Armenante, Marco Euclide

Titel

Development of a Practical Manufacturing Process to Relebactam via Thorough Understanding of the Origin and Control of Oligomeric Impurities

Ist Teil von

• Organic process research & development, 2021-10, Vol.25 (10), p.2249-2259

Ort / Verlag

American Chemical Society

Erscheinungsjahr

2021

Link zum Volltext

Quelle

Alma/SFX Local Collection

Beschreibungen/Notizen

• The development of a robust manufacturing process to relebactam, a potent β-lactamase inhibitor, is described. The origin and control strategy of oligomer impurities formed during hydrogenolysis of benzyl urea intermediate 9 and deprotection of Boc-sulfate intermediate 11 have been thoroughly studied and developed. The optimal manufacturing process has been successfully implemented for commercialization, preparing relebactam (1) in >99% purity with a non-detectable level of oligomers.