Preparation method of thymopentapeptide

A thymus and resin technology, applied in the field of preparation of polypeptide drugs, can solve the problems of long process cycle, complicated process, troublesome crude product refining, etc., and achieve the effect of simple and easy method.

Inactive Publication Date: 2006-06-21
上海丽珠制药有限公司
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

3. In the method introduced in the literature, after the synthesis of the protected TP-5 resin and before obtaining the crude product of TP-5, two steps of cutting off the TP-5 from the resin by TFA first removing the side chain and then using saponification , the process is more complicated and the process cycle is long, which is determined by the specific resin used in this method
Moreover, the acidification after saponification causes NaCl to be brought into the crude product as an impurity, which brings troubles to the refining of the crude product.

Method used

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  • Preparation method of thymopentapeptide

Examples

Experimental program
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Effect test

Embodiment 1

[0039] Use 10Mm Wang resin as raw material.

[0040] Fmoc-Tyr(tBu)-Wang resin preparation:

[0041] Take a dry 250ml eggplant-shaped bottle and add the resin to it, the resin is CH 2 Cl 2 After soaking for half an hour, use CH 2 Cl 2 Wash 3 times and drain;

[0042] Weigh 22.98g of Fmoc-Tyr(tBu)-OH, dissolve it in DMF, add 7.65g HOBT, add 1.22g DMAAP after it is fully dissolved, and add it to the resin after dissolution;

[0043] After adding 50ml DIC / DMF (1mM / ml) to the resin, adjust the pH to 6.5 with pyridine, seal and react at 30°C for 24 hours;

[0044] After the reaction, use CH 2 Cl 2 , EtOH, DMF wash the resin, each wash 3 times;

[0045] Solid phase peptide:

[0046] Dipeptide: Fmoc-Val-Tyr(tBu)-Wang resin;

[0047] Weigh 10mMFmoc-Tyr(tBu)-P into a 250ml eggplant-shaped bottle, soak, and 2 Cl 2 Wash 3 times and drain;

[0048] Deprotection: Add 25% hexahydropyridine / DMF80ml to the resin, 20 minutes at 30°C.

[0049] Washing: CH 2 Cl 2 DMF CH 2 Cl 2 ...

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Abstract

The invention discloses a preparation method of thymopentin. The present invention uses Wang resin as a solid phase carrier to react with fluorenylmethoxycarbonyl-protected tyrosine to generate tyrosine resin, which is used as a starting material, and then sequentially condensed with fluorenylmethoxycarbonyl (Fmoc)-protected amino acids After reacting to generate the protected TP-5 resin, the side chain protecting group and TP-5 are simultaneously cut off from the resin by trifluoroacetic acid cleavage to obtain the crude product of TP-5. The method conditions of the present invention are relatively mild, the method of deprotection is simple and easy, and no by-product DCU is precipitated during the condensation process, which is convenient for washing the resin, improves the condensation yield, reduces the mixing of impurities, and is beneficial to the purification of the product; the present invention On the basis of obtaining the target object with guaranteed quality and quantity, its superiority is reflected in the simplification of the process, the saving of the process, and the simplification of the operation.

Description

technical field [0001] The invention relates to a preparation method of polypeptide drugs, in particular to a preparation method of Thymopentin. Background technique [0002] Thymus is an endocrine organ. Thymic epithelial cells synthesize and secrete a series of polypeptide hormones, which regulate the differentiation and maturation of T lymphocytes. A variety of single polypeptide compounds have been isolated from thymus hormones, such as thymopoitin II (Thymopoitin II), which consists of 49 amino acids, and other thymosin α 1 (Thymsinα 1 ), serum thymus factor (FTS), thymus humoral factor (TMF), among which thymopoietin II is the most studied. The separation of thymopoitin (Thymopoitin) reported by Goldstein G et al. is based on their interest in myasthenia gravis. They found that the biologically active polypeptide can also induce bone marrow cells to differentiate into mature T cells in vitro, so it is speculated that it It is a preparation with important physiologic...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07K7/06C07K14/66
Inventor 杨玉华顾涵英
Owner 上海丽珠制药有限公司
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