The process for preparing octreotide and derivatives thereof

Details The process for preparing octreotide and derivatives thereof The process for preparing octreotide and derivatives thereof

C - Chemistry, Metallurgy

07

K

C07K 7/06 (2006.01) C07K 1/04 (2006.01) C07K 7/08 (2006.01) C07K 14/655 (2006.01)

Patent

CA 2309312

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)

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