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Preparing process for synthesizing oxytocin from solid-phase polypeptide

A solid-phase peptide synthesis, oxytocin technology, applied in the preparation methods of peptides, chemical instruments and methods, peptides, etc., can solve the problems of poor quality, long reaction time and high cost

Active Publication Date: 2007-07-04
SHANGHAI SOHO YIMING PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

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 capacity, the process is complicated, the cost is high, the environment is polluted seriously, and the quality is poor, so it cannot meet the clinical needs.

Method used

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  • Preparing process for synthesizing oxytocin from solid-phase polypeptide

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Experimental program
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Embodiment 1

[0088] Peptide chain preparation:

[0089] Swelling and uncapping:

[0090] Weigh 50 g of Rink Amide resin (200 mesh, 0.93 mmol / g, 46.5 mmol), soak it in 800 ml of DMF for 30 minutes to fully swell the resin, and dry it with nitrogen gas. Add 800 ml of DMF solution with a weight concentration of 20% hexahydropyridine, 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.

[0091] Preparation of Fmoc-Gly-resin:

[0092] 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.

[0093] Preparation of Fmoc-Leu-Gly-resin:

[0094] Add 500 ml of 20% hexahydropyridine in DMF and shake at 25°C for...

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Abstract

The invention discloses a method for preparing oxytocin through solid phase polypeptide synthesis, comprising following steps: taking Rink Amide resin (comprising Rink Amide MBHA resin, Rink Amide Am resin) as raw material, taking amino acid protected by Fmoc, TBTU or HBTU / HOBt as condensing agent, making up amino acid in sequence; adding peptide cutting agent for peptide cutting, adding for precipitation and getting reduced coarse product; adding basic matter, feeding air for oxidation or oxiding with H2O2 with pH being 7.5- 10.0, getting oxidized coarse product; separating and purifying by using C18 or C 8 column and getting final product. The method is characterized by low production cost, simple process, little pollution, high production rate and convenience for industrial production.

Description

technical field [0001] The invention relates to a preparation method of oxytocin, in particular to a preparation method of solid-phase polypeptide synthesis of oxytocin. Background technique [0002] Oxytocin, also known as oxytocin, English name is Oxytocin, structural formula: [0003] [0004] The molecular formula is: C 43 h 66 N 12 o 12 S 2 , the molecular weight is 1007.2. [0005] Oxytocin is a polypeptide hormone uterotonic drug. Has the following functions: [0006] (1) Stimulate the contraction of uterine smooth muscle, simulating the uterine contraction of normal childbirth, resulting in cervical dilatation, and the uterine response to oxytocin gradually increases during pregnancy and reaches its peak at full term. (2) Stimulate the smooth muscle contraction of the mammary gland, which helps the milk to be discharged from the breast, but does not increase the milk secretion of the mammary gland. It takes effect 3 to 5 minutes after intramuscular inject...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K1/00C07K7/00C07K7/16
Inventor 周逸明
Owner SHANGHAI SOHO YIMING PHARMA
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