Preparation method of thymopentapeptide

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...

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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.

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