Process for synthesis of thymopentin

A peptide synthesis and thymus technology, applied in the direction of peptides, etc., can solve the problems of low product purity, poor product solubility, high price of fluorenyl moxycarbonyl derivatives, etc., and achieve the effect of cost reduction and simple purification and separation

Inactive Publication Date: 2006-10-11
CHONGQING HUAPONT PHARMA
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  • Summary
  • Abstract
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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...

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] The synthesis of embodiment 1 Thymopentin

[0032] 1) Protected dipeptide (Val-Tyr(Bu t )-OBu t ) Synthesis of (II)

[0033] Take Z-Val 50.2g, NH 2 -Tyr(Bu t )-OBu t Put 58.6g in a 1L three-neck flask, add 600ml of dichloromethane, cool in an ice bath to 10°C, stir, and add dropwise a dichloromethane solution of 41.2g of dicyclohexylcarbodiimide (DCC). Keep the room temperature after the dropwise addition, stir and react for 8 hours, filter, wash the filtrate with dilute citric acid, dilute sodium carbonate solution, and water successively, separate the organic phase, dry it with anhydrous magnesium sulfate, and recover the solvent under reduced pressure to obtain Z-Val- Tyr(Bu t )-OBu t .

[0034] Z-Val-Tyr(Bu t )-OBu t Dissolve in ethanol, add 5% palladium carbon 5g, pass through hydrogen, and react at room temperature for 3 hours. Palladium carbon was recovered by filtration, the filtrate was evaporated to dryness, and the reaction product was crystallize...

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PUM

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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...

Claims

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Application Information

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IPC IPC(8): C07K7/06
Inventor 谢文全熊伟邹长忠刘汉光
Owner CHONGQING HUAPONT PHARMA
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