Solid phase polypeptide synthesis preparation method for terlipressin

Abstract

The invention discloses a Telis-vasophysin preparing method of solid-phase polypeptide, which comprises the following steps: adopting Rink Amide resin (concluding Rink Amide MBHA resin, Rink AmideAM resin) as original material, Fmoc protective amino acid as monomer, TBTU or HBTU-to-HOBt as condensing agent to connect amino sequently; using Boc-Gly-OH for the last peptide chain; adding peptide cutting agent to cut peptide; adding ether to deposit to obtain crude product; adding alkali material to oxidate at 7.5-10.0 pH value to generate oxide crude product; proceeding separation and purifying through C18 (or C8) pillar to produce object product. The method possesses low manufacturing cost, simple technology, high obtaining rate and low environmental pollution, which is convenient to do industrial construction.

Description

technical field

[0001] The invention relates to a preparation method of terlipressin, in particular to a preparation method of solid phase polypeptide synthesis terlipressin. Background technique

[0002] Terlipressin, English name is Terlipressin, structural formula:

[0003]

[0004] The molecular formula is: C 52 h 74 N 16 o 15 S 2 , the molecular weight is 1227.4. Terlipressin is clinically used for the treatment of severe acute esophageal variceal rupture and bleeding, severe acute gastric and duodenal ulcer bleeding, acute erosive gastritis or hemorrhagic gastritis, adjuvant treatment of pancreas, gallbladder and intestines, and diabetic ketosis Adjunctive treatment of acidosis.

[0005] At present, terlipressin is an artificially synthesized triglycine-lysine-vasopressin, which is a synthetic analog of vasopressin and has no activity itself. After 3 glycyl residues, it slowly converts into active lysine vasopressin, which is used to treat acute esophageal v...

Images