Heating solid-phase synthetic method of polypeptides

A solid-phase synthesis and condensation technology, applied in the preparation methods of peptides, chemical instruments and methods, peptides, etc., to achieve the effect of shortening the reaction time

Inactive Publication Date: 2017-12-29
CS BIO SHANGHAI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The object of the present invention is to provide a kind of polypeptide heating solid-phase synthesis method, to solve many problems in the prior art

Method used

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  • Heating solid-phase synthetic method of polypeptides

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041] Embodiment 1: the preparation method of Ala-Ala-Lys-Lys-Ala-Ala-Lys-Lys-Ala-Lys (CS01)

[0042] (1) Heating and condensing amino acids: add polypeptide resin, Fmoc-protected amino acids, condensing agents and solvents to the reactor, heat to the reaction temperature, and the reaction time is 10-30min. After the reaction, use N,N- Wash the resin 3 times with dimethylformamide, each elution time is 20-40s;

[0043] In this embodiment, the reactor is a 3-channel reactor;

[0044] Polypeptide resin is Wang resin in the present embodiment;

[0045] Condensing agent is DIC / HOBt in the present embodiment;

[0046] The solvent in this example is N,N-dimethylformamide.

[0047] (2) Removal of Fmoc by heating: add 20% piperidine / N,N-dimethylformamide solution of deprotecting agent, heat to reaction temperature, reaction time 2-5min, after the reaction is completed, use N at the reaction temperature , washing the resin once with N-dimethylformamide, and then washing the resin ...

Embodiment 2

[0056] Embodiment 2: the preparation method of Ile-Asp-Leu-Leu-Gln-Gly-Arg-Thr-Arg-Asn-Arg-Cys (CS02)

[0057](1) Heating and condensing amino acids: add polypeptide resin, Fmoc-protected amino acids, condensing agents and solvents to the reactor, heat to the reaction temperature, and the reaction time is 10-30min. After the reaction, use N,N- Wash the resin 3 times with dimethylformamide, each elution time is 20-40s;

[0058] In this embodiment, the reactor is a 3-channel reactor;

[0059] Polypeptide resin is chlorine resin in the present embodiment;

[0060] Condensing agent is DIC / HOAt in the present embodiment;

[0061] The solvent in this example is N,N-dimethylformamide.

[0062] (2) Removal of Fmoc by heating: add 20% piperidine / N,N-dimethylformamide solution of deprotecting agent, heat to reaction temperature, reaction time 2-5min, after the reaction is completed, use N at the reaction temperature , washing the resin once with N-dimethylformamide, and then washing...

Embodiment 3

[0072] The preparation method of Ala-Tyr-Arg-Ala-Ile-Arg-His-Ile-Pro-Arg-Arg-Ile-Arg-Gln (CS03)

[0073] (1) Heating and condensing amino acids: add polypeptide resin, Fmoc-protected amino acids, condensing agents and solvents to the reactor, heat to the reaction temperature, and the reaction time is 10-30min. After the reaction, use N,N- Wash the resin 3 times with dimethylformamide, each elution time is 20-40s;

[0074] In this embodiment, the reactor is a 3-channel reactor;

[0075] In this embodiment, the polypeptide resin is an amino acid resin;

[0076] Condensing agent is DIEA / HBTU in the present embodiment;

[0077] The solvent in this example is chloroform.

[0078] (2) Removal of Fmoc by heating: add 20% piperidine / N,N-dimethylformamide solution of deprotecting agent, heat to reaction temperature, reaction time 2-5min, after the reaction is completed, use N at the reaction temperature , washing the resin once with N-dimethylformamide, and then washing the resin o...

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Abstract

The invention relates to the technical field of synthesis of polypeptides, in particular to a heating solid-phase synthetic method of polypeptides. In heating solid-phase synthesis of polypeptides, all reactions are performed after temperature is raised to a constant value. Compared with traditional solid-phase synthetic methods of polypeptides, the heating solid-phase synthetic method of polypeptides has greatly shortened reaction time and increased reaction speed; compared with microwave solid-phase synthetic methods of polypeptides, the heating solid-phase synthetic method of polypeptides can gain decreased chances for side effects and increased reaction yield of long-chain polypeptides.

Description

technical field [0001] The invention relates to the technical field of polypeptide synthesis, in particular to a method for heating and solid-phase synthesis of polypeptides. Background technique [0002] Generally speaking, a polypeptide refers to a compound composed of 6-40 amino acids, which has a variety of biological activities. At the same time, almost all cells are also regulated by polypeptides, which involve various fields such as hormones, nerves, cell growth and reproduction. They are important chemical messengers that communicate information between cells and organs, and perform their delicate information transmission functions through endocrine, neuroendocrine, and even neurosecretion. [0003] Due to the many advantages of peptide drugs, more and more pharmaceutical companies have invested manpower and financial resources in the research and development of peptide drugs. At present, almost all polypeptide drugs are synthesized by solid-phase synthesis method,...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K1/04C07K1/06
Inventor 王为张恒维朱国基施学庚巢庆
Owner CS BIO SHANGHAI
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