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Method for synthesizing mono pegylation-thymopentin by solid phase and liquid phase combination

A technology of PEGylation and solid-phase synthesis, which is applied in chemical instruments and methods, carrier binding/immobilization of peptides, peptides, etc., to achieve the effect of accurate structure, good mass production basis, and mature synthesis route.

Active Publication Date: 2010-10-27
LANZHOU UNIVERSITY
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  • Abstract
  • Description
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Problems solved by technology

Therefore, TP5 can only be administered by frequent injection or intravenous infusion, which brings great pain and mental stress to the patient.

Method used

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  • Method for synthesizing mono pegylation-thymopentin by solid phase and liquid phase combination
  • Method for synthesizing mono pegylation-thymopentin by solid phase and liquid phase combination
  • Method for synthesizing mono pegylation-thymopentin by solid phase and liquid phase combination

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Embodiment Construction

[0022] A method for synthesizing PEGylated Thymopentin with a solid-liquid phase method, the steps of which are divided into:

[0023] a. The monomethoxypolyethylene glycol modification (mPEG-SCM) was connected to the side chain amino group of α-amino-protected lysine (ε-NH 2 ); 400mg of fluorenylmethoxycarbonyl-protected lysine hydrochloride (Fmoc-lys-OH.HCl) reacted with 700mg of monomethoxypolyethylene glycol modification (mPEG-SCM), and the reaction system was 6ml of chloroform and 24ml of dioxane; 800 μl of diisopropylethylamine (N, N-Diisopropylsilane, referred to as DIEA) was added dropwise at room temperature to keep the pH at 9.0, stirred by magnetic force, and reacted overnight; Add 40mL of water to dissolve, filter out water-insoluble matter, dialyze with a dialysis bag (MW, 3500) for 48 hours, and freeze-dry to obtain 600mg of white powder (Fmoc-lys(PEG)-OH), with a yield of 78.5%.

[0024] The NMR data of the product are as follows:

[0025] 1 H-NMR (DMSO) 7.31...

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Abstract

The invention relates to a method for synthesizing mono pegylation-thymopentin (mPEG-TP5) by solid phase and liquid phase combination. The method comprises the following steps of: connecting modified polyethylene glycol (mPEG-SCM) to side chain amino of lysine protected by amino by adopting liquid-phase synthesis technology; synthesizing mPEG-TP5 by adopting solid-phase synthesis technology; analyzing and purifying high-efficiency liquid phase through dialysis; and identifying the product structure through nuclear magnetism and mass spectrum. The mono pegylation-thymopentin synthesized by themethod improves the defect that the conventional parent medicament thymopentin has quick biodegradation, poor digesting stability, short biological half-life and the like, and has good application prospect.

Description

technical field [0001] The invention relates to the synthesis of PEGylated Thymopentin by adopting a liquid-phase and solid-phase synthesis technique. Background technique [0002] Thymopentin (Thymopentin, TP5) is a synthetic small molecule peptide consisting of 5 amino acid residues, which has the same biological activity as endogenous thymopoietin II in regulating the immune balance of the body. For a variety of immune dysfunction or hypofunction, TP5 can make the immune function tend to normal through the two-way regulation of promotion or inhibition. At present, it has been widely used clinically, and can be used for the treatment of: (1) malignant tumor; (2) chronic hepatitis; (3) surgery and severe infection; (4) diabetes; (5) autoimmune disease; (6) menopause syndrome; (7) aging and frailty, etc. However, TP5 is quickly degraded by protease and aminopeptidase after injection into the human body, and the half-life of the drug prototype is only 30 seconds. However, ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K17/08
Inventor 倪京满王锐王长林李倩
Owner LANZHOU UNIVERSITY
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