Process for preparing octreotide and derivatives thereof

US6476186B1 · kind B1 · utility

Assignee

• INSTITUTE OF NUCLEAR ENERGY RESEARCH · TW

Inventors

• Yao-Tsung HSIEH
• Shiang-Rong Chang · 溪州鄉, TW
• Shyh-Yi Chyi · 溪州鄉, TW
• Hui-Lan Wu
• Shu-Ling Chen · Taipei, TW
• Henton Huang · 溪州鄉, TW
• Te-Wei Lee · Daxi District, TW
• Tian-Fu Huang · 溪州鄉, TW

Key dates

• Filing date: May 24, 2000
• Grant date: Nov 5, 2002
• Expiry date: May 24, 2020

Classification

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

Abstract

This invention relates a process for preparing octreotide and derivatives thereof. The starting material, Thr(ol)(tBu)-2-chlorotrityl resin is coupled with the various amino acids. The straight peptide-resin of D-Phe-Cys(Trt)-Phe-D-Trp(Boc)-Lys(Boc)-Thr(tBu)-Cys(Trt)-Thr(ol)(tBu)-2-chlorotrityl resin or D-Phe-Cys(Trt)-Tyr(tBu)-D-Trp(Boc)-Lys(Boc)-Thr(tBu)-Cys(Trt)-Thr(ol)(tBu)-2-chlorotrityl resin was obtained. Cleavage of the peptide from the resin was achieved by strong acid solution. The cleaved peptide reacted with charcoal to give disulfide-containing peptide of