Process for the preparation of cyclo(Asp-DPhe-NMeVal-Arg-Gly)

US6822074B1 · kind B1 · utility

Assignee

• Merck Patent GmbH · DE

Inventors

• Alfred Jonczyk · Darmstadt, DE
• Markus Arnold · Neu-Isenburg, DE

Key dates

• Filing date: Sep 12, 2001
• Grant date: Nov 23, 2004
• Expiry date: Sep 12, 2021

Classification

• Technology area (CPC Y): Emerging Cross-Sectional Technologies
• CPC primary: Y02P20/55
• WIPO field: Biotechnology
• WIPO sector: Chemistry

Abstract

Process for the preparation of the cyclic pentapeptidecyclo(Arg-Gly-Asp-DPhe-NMeVal)by cyclization of a linear pentapeptide selected from the group consisting ofH-Arg(Pbf)-Gly-Asp(OBzl)-DPhe-NMeVal-OH,H-Gly-Asp(OBzl)-DPhe-NMeVal-Arg(Pbf)-OH,H-Asp(OBzl)-DPhe-NMeVal-Arg(Pbf)-Gly-OH,H-DPhe-NMeVal-Arg(Pbf)-Gly-Asp(OBzl)-OH orH-NMeVal-Arg(Pbf)-Gly-Asp (OBzl)-DPhe-OH,subsequent protective group removal and, if appropriate, further conversion into its physiologically acceptable salts.