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Liquid phase spherical carrier, and preparation method and applications thereof

A spherical carrier and a carrier technology, which are applied in the field of liquid-phase spherical carriers and their preparation, can solve the problems of increased steric hindrance of polypeptides, inability to effectively monitor the surface substituents of solid-phase synthetic carriers, affecting reaction efficiency, etc., and achieve low steric hindrance. , the effect of facilitating industrial production and application

Inactive Publication Date: 2019-07-09
HYBIO PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] The substituents on the surface of the solid-phase synthesis carrier cannot be effectively monitored, the particle size distribution of the carrier is uneven, and the surface of the carrier collapses, which affects the reaction efficiency. As the peptide chain grows, the steric hindrance of the polypeptide on the surface of the solid-phase carrier increases.

Method used

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  • Liquid phase spherical carrier, and preparation method and applications thereof
  • Liquid phase spherical carrier, and preparation method and applications thereof
  • Liquid phase spherical carrier, and preparation method and applications thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0047] The synthesis of embodiment 1 compound A

[0048]

[0049] Take compound 1 (C 60 Cl 6 ) 5.6 grams (6mmol) and p-hydroxymethylphenol 7.4 grams (60mmol) were added in the 500mL there-necked flask, then in the reaction flask, DMF (100mL) was added, stirred evenly, then 8.3 grams of potassium carbonate (60mmol) was added. The temperature of the reaction solution was raised to 80° C. and stirring was continued for 16 hours. The reaction was monitored by HPLC. After the raw materials were consumed, the reaction solution was cooled in an ice bath to below 10°C. Under the condition of sufficient stirring, 1 mol / L dilute hydrochloric acid (100 mL) and purified water (200 mL) were slowly added dropwise to the reaction liquid, and stirring was continued for half an hour after the dropwise addition was completed. After the solid precipitated, it was filtered, and the filter cake was washed with purified water (100 mL) and diethyl ether (100 mL) successively. Vacuum drying w...

Embodiment 2

[0050] The synthesis of embodiment 2 compound B

[0051]

[0052] Take 4.7 g (5 mmol) of compound 1 and 12.9 g (50 mmol) of compound 2 into a 1L three-necked flask, then add DMF (150 mL) into the reaction flask, stir well, and then add 6.9 g (50 mmol) of potassium carbonate. The temperature of the reaction solution was raised to 80° C. and stirring was continued for 16 hours. The reaction was monitored by HPLC. After the raw materials were consumed, the reaction solution was cooled in an ice bath to below 10°C. Under the condition of sufficient stirring, 1 mol / L dilute hydrochloric acid (100 mL) and purified water (150 mL) were slowly added dropwise to the reaction liquid, and stirring was continued for half an hour after the dropwise addition was completed. After filtering, the filter cake was washed with purified water (100 mL) and diethyl ether (100 mL) successively. Vacuum drying at 60° C. for 5 hours gave 8.8 g of light yellow solid compound 3 with a yield of 90%. ...

Embodiment 3

[0056] The synthesis of embodiment 3 compound C

[0057]

[0058] Take compound 1 6.6 grams (7mmol) and Fmoc-NH 2 Add 16.7 grams (70 mmol) into a 1L three-neck flask, then add DMF (150 mL) into the reaction flask, stir evenly, and then add 6.9 grams (50 mmol) of potassium carbonate. The temperature of the reaction solution was raised to 80° C. and stirring was continued for 16 hours. The reaction was monitored by HPLC. After the raw materials were consumed, the reaction solution was cooled in an ice bath to below 10°C. Under the condition of sufficient stirring, 1 mol / L dilute hydrochloric acid (100 mL) and purified water (150 mL) were slowly added dropwise to the reaction liquid, and stirring was continued for half an hour after the dropwise addition was completed. After filtering, the filter cake was washed with purified water (100 mL) and diethyl ether (100 mL) successively. Vacuum drying at 60° C. for 5 hours gave 12.5 g of brown solid compound 6 with a yield of 92...

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Abstract

The invention relates to a liquid phase spherical carrier, and a preparation method and applications thereof, and more specifically discloses a spherical carrier can be used for liquid phase synthesis. The spherical carrier possesses a structure represented by formula I, wherein R is used for representing a functional group selected from groups containing hydroxyl, amino, carboxyl, or halogen preferably. The liquid phase synthesis carrier can be used for liquid phase synthesis of polypeptides. The preparation method is simple; and synthesis efficiency is high.

Description

technical field [0001] The invention relates to the field of polypeptide synthesis, in particular to a liquid-phase spherical carrier and its preparation method and application. Background technique [0002] Peptide synthesis has a history of more than 100 years, and at this stage there are mainly traditional solid-phase synthesis methods and liquid-phase synthesis methods. Both types of methods have different disadvantages. The traditional liquid-phase synthesis method has many disadvantages, such as many reaction steps, difficult separation methods, cumbersome post-treatment, and long synthesis cycle; after each peptide inoculation, it must be separated and purified or crystallized to remove unreacted raw materials or by-products of the reaction. It is quite time-consuming and troublesome, and the loss caused by the operation is also great; in order to overcome these shortcomings, Merrifield first developed the method of solid-phase peptide synthesis in 1963. The method ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C43/253C07C41/16C07C217/58C07C213/08C07K1/04C07K1/02C07K1/06C07K14/815
CPCC07C43/253C07C217/58C07K1/02C07K1/042C07K1/06C07K14/815C07C41/16C07C213/08C07K1/04Y02P20/55
Inventor 陈新亮宓鹏程潘俊锋袁建成
Owner HYBIO PHARMA
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