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Solid-phase resin and its preparation method and use

A technology of resin and peptide resin, which is applied in the field of peptide solid-phase synthesis, can solve the problems of high cost and unfavorable large-scale production of PEG king resin

Active Publication Date: 2014-07-30
HAINAN SHUANGCHENG PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, DKP is still not well controlled, and the cost of PEG king resin is very high, which is not conducive to mass production

Method used

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  • Solid-phase resin and its preparation method and use
  • Solid-phase resin and its preparation method and use
  • Solid-phase resin and its preparation method and use

Examples

Experimental program
Comparison scheme
Effect test

preparation example Construction

[0059] Resin preparation method

[0060] The above-mentioned specific resin that connects an amino acid or a small peptide in the HMPA Linker and AM resin provided by the present invention can be obtained by polypeptide solid-phase synthesis. Specifically, the following steps may be included:

[0061] Step 1. Obtain peptide resin fragments by peptide solid-phase synthesis: AA 1 -AA 2 ...AA n - AM resin;

[0062] Step 2. Connect HMPA Linker to get HMPA-AA 1 -AA 2 ...AA n - AM resin.

[0063] The condensing agent used in the above step 2 is preferably DIC / HOBt.

[0064] The use of resin - a new preparation method of thymus method

[0065] The above-mentioned specific resin that connects an amino acid or a small peptide in the HMPA Linker and AM resin provided by the present invention can be used for the new solid-phase synthesis of polypeptides by thymus method.

[0066] The preparation method of the thymus method new polypeptide solid-phase synthesis provided by the i...

Embodiment 1

[0098] H-[Arg(Pbf)] 4 -Synthesis of AM resin

[0099] (1) AM resin (manufactured by Tianjin Nankai Hecheng Technology Co., Ltd., with a substitution degree of 1.1mmol / g, 100g) was put into a solid-phase reaction column, washed twice with DMF, and swelled in DMF for 30 minutes.

[0100] (2) Dissolve Fmoc-Arg(Pbf)-OH (142.73g) and HOBt (44.58g) in DMF (800mL), add DIPCDI (69mL), and pre-react in an ice bath for 10 minutes.

[0101] (3) Add the above reaction solution into a solid-phase reaction kettle, stir it mechanically, and react at room temperature for 3 hours. The ninhydrin test shows that the resin is colorless and transparent.

[0102] (4) Drain the solution and wash 3 times with DMF. Use 20% piperidine in DMF to remove Fmoc twice at room temperature for 10 min and 20 min respectively.

[0103] (5) The solution was drained, the resin was washed 5 times with DMF and 2 times with DCM, and the ninhydrin test was positive.

[0104] (6) Repeat step (2) to step (5) to obta...

Embodiment 2

[0106] H-Asn(Trt)-HMPA-[Arg(Pbf)] 4 -Synthesis of AM resin

[0107] (1) Dissolve HMPA Linker (40.08g) and HOBt (44.58g) in DMF (800mL), add DIPCDI (69ml), and pre-react in an ice bath for 10 minutes.

[0108] (2) The above reaction solution was added to a solid-phase reaction column, stirred mechanically, and reacted at room temperature for 3 hours, and detected by ninhydrin, the resin was colorless and transparent. The solution was drained, and the resin was washed 3 times with DMF.

[0109] (3) Dissolve Fmoc-Asn(Trt)-OH (131.27g), HOBt (44.58g), and DMAP (2.69g) in DMF (6L), add DIPCDI (69ml), and pre-react in an ice bath for 10 minutes .

[0110] (4) The above reaction solution was added to a solid-phase reaction column, stirred mechanically, and reacted at room temperature for 3 hours. Drain the solution, wash the resin 3 times with DMF, and shrink with methanol.

[0111] (5) Block with resin for 2 hours, and the blocking solution is DMF / acetic anhydride / pyridine=1L / 8...

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Abstract

The invention discloses solid-phase resin and its preparation method and use. The solid-phase resin has a structure shown in the formula I of HMPA-AAn-AM resin I. In the formula I, AA represents the same or different side chain-protection amino acids such as Arg, Lys, Asn, Gln, Asp, Glu, Pro and Gly, and n represents an integer of 0-8. The solid-phase resin can be used for thymalfasin solid-phase synthesis.

Description

technical field [0001] The invention relates to the field of polypeptide solid-phase synthesis, in particular to a novel solid-phase synthesis method of the thymus method. Background technique [0002] Thymus fasin is a polypeptide composed of 28 amino acids, its sequence is: Ac-Ser-Asp-Ala-Ala-Val-Asp-Thr-Ser-Ser-Glu-Ile-Thr-Thr-Lys-Asp- Leu-Lys-Glu-Lys-Lys-Glu-Val-Val-Glu-Glu-Ala-Glu-Asn. Its molecular formula is: C 129 h 215 N 33 o 55 , molecular weight 3108.37. [0003] Thymus Actin formerly known as thymosin α1, also known as thymosin α1 or Tα1. Thymofasin is a kind of thymosin. Thymosin is a group of physiologically active polypeptides secreted by thymus tissue, which can promote lymphocyte transformation, enhance macrophage phagocytosis, and can be used to treat various immunodeficiency diseases. Clinical studies have shown that thymosin α1 is the most important and most biologically active component of thymosin. Thymofasin has significant two-way immunoregul...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K14/575C07K1/06C07K1/04
CPCY02P20/55C07K14/57581
Inventor 张巍袁剑琳张成广谭松暖陈超
Owner HAINAN SHUANGCHENG PHARMA
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