Process for synthesis of thymopentin

Abstract

This invention is about the synthesis of thymic-pentapeptide. Using tyrosine and its derivative as raw material, after four condensation reactions, we add valine with tertiary-butyl or tertiary-butyl ketonic oxygen group protection, aspartate, lysine, and arginine accordingly to obtain protected pentapeptide. With the method we reported here, the all protection groups could be removed once to obtain targeted products, due to our adoption of tertiary-butyl ketonic oxygen group protection strategy. The method is advantageous in simplified procedure, high yield, cost cutting and high purity.

Description

Technical field: [0001] The invention relates to a synthetic method of thymopentin. Background technique: [0002] Thymopentin is the 32-36th amino acid residue fragment of thymopoietin II (Thymopoietin II), and its basic sequence is NH 2 -Arg-Lys-Asp-Val-TYr-OH, retains potent bioactivity of thymopoietin. Thymopentin is a cellular immunomodulatory drug that can induce T cell differentiation, promote the development and activation of T lymphocyte subsets, and can be used to treat malignant tumors, hepatitis, and autoimmune diseases. [0003] Many documents have reported the method for preparing thymopentin by liquid phase synthesis technology, such as the method disclosed in CN1442428A, MI91A-000706 is to use tyrosine derivatives as raw materials, carry out multiple condensation reactions, respectively connect successively by tert-butyl, tert-butyl Valine, aspartic acid, and lysine protected by protective groups such as butoxycarbonyl generate protected tetrapeptides. When...

AI Technical Summary

Problems solved by technology

[0005] 1. If fluorenylmethoxycarbonyl is used as a protecting group, the production cost is high because of the high price of fluorenylmethoxycarbonyl derivatives;

[0006] 2. If benzyloxycarbonyl is used as a protecting group, the resulting product has poor solubility, and most solvents cannot dissolve it. Only DMF can be selected as the solvent, and it is in the form of jelly, which cannot be filtered, making the purification of the product very difficult. , the product purity obtained is also very low;