Solid phase polypeptide synthesis preparation method for terlipressin

A technology for solid-phase peptide synthesis and terlipressin, which is applied to the preparation methods of peptides, oxytocin/vasopressin, chemical instruments and methods, etc., can solve the problems of low yield, complex process and long reaction time And other issues

Active Publication Date: 2006-11-22
SHANGHAI SOHO YIMING PHARMA
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  • Abstract
  • Description
  • Claims
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Problems solved by technology

Because the three wastes of this process are relatively serious, the yield is also low, the reaction time is long, there is no large-scale production cap

Method used

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  • Solid phase polypeptide synthesis preparation method for terlipressin

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Embodiment 1

[0108] Peptide chain preparation:

[0109] Swelling and Capping:

[0110] Weigh 50 g of Rink Amide resin (200 mesh, 0.93 mmol / g, 46.5 mmol), soak it in 800 ml of DMF to fully swell the resin, and dry it with nitrogen gas. Add 800 ml of 20% hexahydropyridine in DMF and shake at 25°C for 30 minutes. Hexahydropyridine was blown and filtered with nitrogen, washed with DMF, anhydrous methanol, and DMF three times respectively, and dried with nitrogen.

[0111] Preparation of Fmoc-Gly-resin:

[0112] Add Fmoc-Gly-OH (MW: 297.3, 186mmol) 55.3g, TBTU or HBTU (MW: 321, 186mmol) 59.7g, HOBT (MW: 153.1, 186mmol) 32.7g, NMM 41.4ml (MW = 101.2), 400ml DMF , and the mixture was shaken at 25°C for 1 hour. Blow dry with nitrogen, wash with DMF, anhydrous methanol, and DMF three times each, and blow dry with nitrogen.

[0113] Preparation of Fmoc-Lys(Boc)-Gly-resin:

[0114] Add 500 ml of 20% hexahydropyridine in DMF and shake at 25°C for 30 minutes. Blow dry with nitrogen, wash with DM...

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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...

Claims

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Application Information

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IPC IPC(8): C07K7/16C07K1/04C07K7/52
Inventor 周达明
Owner SHANGHAI SOHO YIMING PHARMA
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