Liquid-phase Synthesis Of Somatostatin

Somatostatin(somatostatin,SST) is a biologically active peptide which has a widespread distribution in vivo.At present,Synthetic Somatostatin has been commercialized and is currently widely used as the treatment of gastrointestinal tract bleeding,esophageal variceal bleeding,Acute Pancreatitis and post-operati -ve complications of acute pancreatitis as well as pancreas,gall bladder and intestinal fistula.Because of its wide range of biological effects,Somatostatin has wide market prospect as a clinical therapeutic drug.Therefore,it is bearing external economic value that designning a simple route which posses simple process,low production cost and meanwhile is suitable for the industrial production to synthesize Somatostatin.The product synthesized by this method has high purity,high yield and good quality.The method of synthesizing Somatostatin was:using Boc/Bzl protect strategy,and dividing the pepetide of Somatostatin into four segments which was tagged as follows from C-terminal of the peptide:fragmentâ… :Thr(Bzl)-Phe-Thr (Bzl)-Ser(Bzl)-Cys(MeOBzl)-OBzl;fragmentâ…¡:Boc-Phe-Trp-Lys(Z)-OH;fragmntâ…¢:Boc-Asn-Phe-OH;fragmentâ…£:Boc-Ala-Gly-Cys(MeOBzl)-Lys(Z)-OH.The full -protected Somatostatin which was then transferred into the reduced Somatosta -tin by removing all the protection groups of the peptide-based chain with triflu -oroacetic acid and anisole was synthesized through the combination of progressi -ve condensation method and fragment condensation method.FolIowing we obtai -ned the crude Somatostatin by the air or oxygen oxidation of the reduceed Soma -tostatin.At last we obtained the pure Somatostatin through Sephades G-25 desalting and HPLC purification.The pure Somatostatin possed right molecule weight {[M+H~+]=1637.8} by HR-MS analysis and has great purity of ee up to 98%by HPLC analysis.