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Purification method of tetracosactide acetate

A technology of ticoctide and purification method, which is applied in the field of polypeptide drug synthesis, can solve the problems of unfavorable large-scale production of ticoctide, complex synthesis process and high production cost, and achieves the improvement of ion pairing ability, the simplification of technological process, and the reduction of Effects of product toxicity

Inactive Publication Date: 2017-03-22
合肥国肽生物科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Currently on the market, the synthesis method of Tecosactide has complex synthesis process, long cycle and high production cost, which is not conducive to the large-scale production of Tecosactide

Method used

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  • Purification method of tetracosactide acetate
  • Purification method of tetracosactide acetate

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] S1, swelling of 2-Cl-Resin

[0026] Weigh 1g of 2-Cl-Resin and add it into the peptide synthesis reactor from the open end, add DCM solution to the peptide synthesis reactor to immerse 2-Cl-Resin, swell for 30min and drain the solvent;

[0027] Among them, the substitution degree of 2-Cl-Resin is 0.64mmol / g;

[0028] S2, Synthesis of Tecocteptide-2-Cl-Resin

[0029] Tecoctide-2-Cl-Resin is:

[0030] Ser(tBu)-Tyr(tBu)-Se(tBu)r-Met-Glu(OtBu)-His(trt)-Phe-Arg(pbf)-Trp(Boc)-Gly-Lys(Boc)-Pro-Val -Gly-Lys(Boc)-Lys(Boc)-Arg(pbf)-Arg(pbf)-Pro-Val-Lys(Boc)-Val-Tyr(tBu)-Pro-2-Cl-Resin

[0031] The protected amino acids used in this example are listed in Table 1 below for the protected amino acids and molecular weights corresponding to the 1-24 amino acids from the resin:

[0032] Table 1

[0033]

[0034] Some commonly used abbreviations in the present invention have the following meanings:

[0035] Fmoc: fluorenylmethoxycarbonyl

[0036] Boc: tert-butoxycarbonyl

[00...

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Abstract

The invention discloses a purification method of tetracosactide acetate. The method comprises the steps of: adopting 2-Cl Resin as the starting resin carrier, conducting solid-phase synthesis, and adopting specific microwave technology reaction to connect corresponding amino acids in a tetracosactide sequence so as to obtain tetracosactide-2-Cl-Resin; carrying out cutting and sedimentation reaction on the tetracosactide-2-Cl-Resin to obtain tetracosactide crude peptide; subjecting the tetracosactide crude peptide to specific reversed-phase high-performance liquid chromatography purification, and performing freeze-drying, thus obtaining a tetracosactide pure product. The method provided by the invention lowers the liquidity pH value to improve the ion pairing ability, is beneficial to purification and purity improvement, also optimizes the purification gradient, shortens the purification time, saves the use of purification mobile phase, and reduces the production cost. Acetic acid is employed to replace trifluoroacetic acid to regulate the PH of the mobile phase, trifluoroacetic acid can be avoided in the final product, the product toxicity is lowered, and the technological process is simplified.

Description

technical field [0001] The invention belongs to the technical field of polypeptide drug synthesis, and in particular relates to a purification method of tecoctide acetate. Background technique [0002] The sequence of Tetracosactide Acetate is: [0003] Ser-Tyr-Ser-Met-Glu-His-Phe-Arg-Trp-Gly-Lys-Pro-Val-Gly-Lys-Lys-Arg-Arg-Pro-Val-Lys-Val-Tyr-Pro-OH, [0004] Its molecular formula is C 136 h 210 N 40 o 31 S, the molecular weight is 2933.46. [0005] Tetracosactide (Tetracosactide) is a synthetic 24-peptide corticotropin analogue, the sequence of amino acids is the same as the amino terminal 24 amino acids of natural corticotropin (human, bovine, pig), and has the same physiological activity. The most prominent feature is that it will not produce antibody reaction under normal circumstances and has no serious side effects, and is especially suitable for patients who have allergic reactions or are ineffective for natural porcine corticotropin. Tecoctide is commonly us...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K14/695C07K1/20C07K1/14C07K1/06C07K1/04
CPCY02P20/55C07K14/695
Inventor 陈为光武兴伟
Owner 合肥国肽生物科技有限公司
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