Phosphorus-containing molecular carrier PPS based target polypeptide liquid-phase synthesis method

A liquid-phase synthesis and small-molecule technology, which is applied to the preparation methods of peptides, chemical instruments and methods, and compounds of Group 5/15 elements of the periodic table, etc. Long time period and other issues, to achieve obvious practical application value, reduce waste pollution, and easy to recycle and reuse

Inactive Publication Date: 2019-10-25
NORTHWESTERN POLYTECHNICAL UNIV
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0011] In order to avoid the deficiencies of the prior art, the present invention proposes a liquid-phase synthesis method for the target polypeptide based on the phosphorus-containing small molecule carrier PSS, which solves the problem that the liquid-phase reaction of the current polypeptide chemical synthesis method is relatively complicated, and the separation steps are many and time-consuming. Long cycle, small purification scale, high production cost, while solid phase reaction has small production scale, expensive raw materials, large waste, many resin wastes and serious environmental pollution problems

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  • Phosphorus-containing molecular carrier PPS based target polypeptide liquid-phase synthesis method
  • Phosphorus-containing molecular carrier PPS based target polypeptide liquid-phase synthesis method
  • Phosphorus-containing molecular carrier PPS based target polypeptide liquid-phase synthesis method

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Embodiment Construction

[0050] The present invention will now be further described in conjunction with the embodiments and drawings:

[0051] The synthesis steps are: (1) Carrier coupling: Use phosphorus-containing small molecule carrier (PSS) instead of solid-phase resin, and under the action of coupling dehydrating agent, it is combined with the first amino acid (PG-AA1-OH) whose amino group is protected. C-terminal connection; (2) Separation and purification: After the reaction is completed, the product A can be separated from other impurities with the help of the phosphate ester carrier to crystallize and precipitate in different solvent systems, after simple filtration and washing or recrystallization Purified A can be obtained by operation; (3) Removal of N-terminal PG: After the product A is treated with a PG removal reagent, the product can be easily crystallized and precipitated in different solvent systems by using the phosphate carrier. B is separated from other impurities, and purified B can...

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Abstract

The invention relates to a phosphorus-containing molecular carrier PPS based target polypeptide liquid-phase synthesis method. By adoption of phosphorus-containing molecular carrier PPS for substituting a resin carrier in solid-phase polypeptide synthesis, polypeptide separation and purification are facilitated, damage after shearing is avoided, and easiness in recycling is achieved. The polypeptide synthesis method integrates advantages of liquid-phase and solid-phase synthesis methods, simplicity, convenience, quickness, saving and high efficiency in large-scale synthesis of polypeptides andderivatives area realized, and the phosphorus-containing molecular carrier can be recovered and reused directly, so that raw material waste can be reduced, waste pollution is reduced, cost saving isrealized, environmental protection is benefited, and an evident practical application value in organic synthesis and polypeptide chemistry is achieved.

Description

Technical field [0001] The invention belongs to the field of organic synthesis and polypeptide chemistry, and relates to a method for liquid phase synthesis of target polypeptides based on a phosphorus-containing small molecule carrier PSS, in particular to phosphoryloxybenzyl alcohols or phosphoryloxybenzaldehyde (or ketone) The oxime derivatives etc. are resin-free peptide synthesis methods with phosphorus-containing small molecule carriers. Background technique [0002] Polypeptides and proteins play a central role in many biological and physiological processes in organisms. They act as hormones, neurotransmitters in cell-to-cell communication, antibodies that protect organisms from foreign invasion, and participate in the passage of various substances through biological membranes. Transportation. Understanding the mechanisms and principles that control the structure and functional properties of biologically active proteins at the molecular level is a major goal of medicinal ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K7/06C07K1/30C07K1/06C07K1/02C07F9/32
CPCC07K7/06C07F9/3282Y02P20/55
Inventor 钦传光晁洁李海迪田广张子鑫李东升
Owner NORTHWESTERN POLYTECHNICAL UNIV
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