Details

Autor(en) / Beteiligte

• Weisenburger, Gerald A
• Anderson, D. Keith
• Clark, Jerry D
• Edney, Albert D
• Karbin, Puneh S
• Gallagher, Donald J
• Knable, Carl M
• Pietz, Mark A

Titel

Pilot-Plant Preparation of an αvβ3 Integrin Antagonist: Process Development of a Carbonyldiimidazole Peptide Coupling

Ist Teil von

• Organic process research & development, 2009-01, Vol.13 (1), p.60-63

Ort / Verlag

American Chemical Society

Erscheinungsjahr

2009

Quelle

Alma/SFX Local Collection

Beschreibungen/Notizen

• The process development of a peptide coupling with CDI is discussed. Various solvents, addition orders, stoichiometries, and reaction temperatures were investigated. A reliable crystallization procedure was also developed. The new process was piloted to provide 342 kg of product in two batches with an average 85% yield and 99% assay.