THE PROCESS FOR PREPARING OCTREOTIDE AND DERIVATIVES THEREOF

THE PROCESS FOR PREPARING OCTREOTIDE AND DERIVATIVES THEREOF

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- chlorotrit yl re...

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Bibliographische Detailangaben
Hauptverfasser: CHEN, SHU-LING, LEE, TE-WEI, HUANG, HENTON, HSIEH, YAO-TSUNG, HUANG, TIAN-FU, CHANG, SHIANG-RONG, WU, HUI-LAN, CHYI, SHYH-YI
Format: Patent
Sprache:eng ; fre
Schlagworte:
CHEMISTRY
METALLURGY
ORGANIC CHEMISTRY
PEPTIDES
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Beschreibung
Zusammenfassung: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- chlorotrit yl resin or D-Phe-Cys(Trt)-Tyr(tBu)-D-Trp(Boc)-Lys(Boc)-Thr(tBu)-Cys(Trt)-Thr(ol)(tBu)-2 - chlor otrityl 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 (see above formula)