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Solid phase polypeptide synthesis preparation method for thymopoietin pentapeptide

A technology of solid-phase peptide synthesis and thymus, which is applied in the preparation method of peptides, chemical instruments and methods, peptides, etc., can solve the problems of high production cost, pollution of three wastes, complicated process, etc., and achieve lower production costs, less pollution of three wastes, Reduce the effect of the three wastes

Active Publication Date: 2006-11-22
SHANGHAI SOHO YIMING PHARMA
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  • Abstract
  • Description
  • Claims
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AI Technical Summary

Problems solved by technology

Low peptide yield, high production cost, complex process, use of highly toxic hydrogen fluoride and trifluoroacetic acid, serious pollution of three wastes, difficult for industrial production

Method used

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Examples

Experimental program
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Embodiment 1

[0054] In the following steps:

[0055] The decapping reagent is: hexahydropyridine:DMF=1:4, volume ratio;

[0056] Said peptide-connecting reagent is: NMM:DMF=1:10; in the peptide-connecting reagent, the mole of TBTU is 3.5 times of the raw resin, and the mole of HOBT is 3.5 times of the raw resin.

[0057] Preparation of Fmoc-Tyr(tBu)-resin:

[0058] Take 50g of CTC resin (1.0mmol / g resin, 50mmol), soak in 800ml of DMF to fully swell the resin, and blow dry.

[0059] 1) Take 20g (FW: 403.4, 50mmol) Fmoc-Tyr(tBu)-OH, 55ml DIPEA, dissolve it in 500ml DMF, put it into a reaction vessel, and react at room temperature for 60 minutes. Add methanol 50ml, react at room temperature for 60 minutes

[0060] 2) Blow dry, wash with DMF, absolute ethanol and DMF respectively three times, and blow dry.

[0061] Preparation of Fmoc-Val-Tyr(tBu)-resin:

[0062] 1) Add 1000ml decapping reagent, react at room temperature for 30 minutes, blow dry, wash with DMF, absolute ethanol and...

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PUM

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Abstract

The invention discloses a preparing method of thymic pentagon through solid-phase polypeptide, which comprises the following steps: (1) adopting CTC resin (or Wang resin) as original material, Fmoc protected amino acid as monomer, TBTU / HOBt (or HBTU / HOBt) as condensing agent to connect amino acid sequently; utilizing Boc-Arg-OH for the last peptide chain; adding the endope cutting agent in the product of step (1) to cut peptide; adding ether to deposit; collecting crude product; (3) adapting C18 or C8 pillar to proceed separating and purifying the crude product in the step (2) to obtain the object product.

Description

technical field [0001] The invention relates to a preparation method of thymopentin, in particular to a solid-phase polypeptide synthesis preparation method of thymopentin. Background technique [0002] Thymopentin, the English name is Thymopoietin pentapeptide; TP-5; Thymopentin, the structural formula is Arg-Lys-Asp-Val-Tyr-OH, molecular formula and molecular weight: C 30 h 49 N 9 o 9 , 679.77. [0003] Thymopentin is clinically used as an immune enhancer, for the early treatment of AIDS, chronic hepatitis, malignant tumors, surgery and severe infection, and can also be used for diabetes, rheumatoid arthritis, lupus erythematosus, glomerulonephritis, multiple sclerosis, etc. Autoimmune diseases, also has anti-aging effects, etc. [0004] Thymopentin was first developed by Johnson & Johnson, and it was launched in Italy and Germany as an immune enhancer and immune regulator in 1985 under the trade name Timunox. [0005] At present, the conventional preparation method ...

Claims

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Application Information

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IPC IPC(8): C07K7/06C07K1/04
Inventor 周达明
Owner SHANGHAI SOHO YIMING PHARMA
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