Pure-solid-phase synthesis method of polypeptide antibiotic Colistin

A technology of solid-phase synthesis and resin synthesis, which is applied to the preparation method of peptides, polymyxin, chemical instruments and methods, etc., can solve the problems of cumbersome steps and large amount of solvent usage, reduce the amount of use, and simplify the synthesis process and steps, the effect of shortening compositing time

Inactive Publication Date: 2013-11-20
HYBIO PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

This method has the disadvantages of cumbersome steps, multiple p

Method used

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  • Pure-solid-phase synthesis method of polypeptide antibiotic Colistin
  • Pure-solid-phase synthesis method of polypeptide antibiotic Colistin

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] Embodiment 1: the preparation of the Fmoc-Thr(Resin)-OAll that the degree of substitution is 0.2mmol / g

[0030] Weigh 100g (100mmol) of DHP HM resin with a substitution degree of 1.0mmol / g, add it to a solid-phase reaction column, wash it twice with DCE, and swell the resin with DCE for 60 minutes, take 22.7g Fmoc-Thr-OAll (60mmol) and 7.5g PPTS (30mmol) was dissolved in 200ml DCM solution, added to the resin, and reacted at 80°C for 5h under the protection of nitrogen. After cooling and filtering, washing with DMF, DCM and Hexane three times respectively, and drying, the detected substitution degree was 0.202 mmol / g.

Embodiment 2

[0031] Embodiment 2: the preparation of the Fmoc-Thr(Resin)-OAll that the degree of substitution is 0.5mmol / g

[0032] Weigh 100g (100mmol) of DHP HM resin with a substitution degree of 1.0mmol / g, add it to a solid-phase reaction column, wash it twice with DCE, and swell the resin with DCE for 60 minutes, take 56.8g of Fmoc-Thr-OAll (150mmol) and 18.8g PPTS (75mmol) was dissolved in 200ml DCM solution, added to the resin, and reacted at 80°C for 5h under the protection of nitrogen. After cooling and filtering, washing with DMF, DCM and Hexane three times respectively, and drying, the detected substitution degree was 0.510mmol / g.

Embodiment 3

[0033] Embodiment 3: the preparation of the Fmoc-Thr(Resin)-OAll that the degree of substitution is 0.3mmol / g

[0034] Weigh 100g (100mmol) of DHP HM resin with a substitution degree of 1.0mmol / g, add it to a solid-phase reaction column, wash it twice with DCE, and swell the resin with DCE for 60 minutes, take 34.1g Fmoc-Thr-OAll (90mmol) and 11.3g PPTS (45mmol) was dissolved in 200ml DCM solution, added to the resin, and reacted at 80°C for 5h under the protection of nitrogen. After cooling and filtering, washing with DMF, DCM and Hexane three times respectively, and drying, the detected substitution degree was 0.308mmol / g.

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Abstract

The invention belongs to the technical field of medicine synthesis, and discloses a method of pure-solid-phase synthesis of polypeptide antibiotic Colistin. By use of the method, the synthetic process and procedure of the Colistin are simplified, the synthesis time is shortened, and the use amount of solvents is reduced.

Description

technical field [0001] The invention relates to the technical field of drug synthesis, in particular to a pure solid phase synthesis method of polypeptide antibiotic Colistin. Background technique [0002] Colistin, molecular formula C 52 h 98 N 16 o 13 ; The relative molecular mass is 1155.45; the CAS registration number is 1264-72-8; its structure is shown in the following formula: [0003] C8H15O-Dab-Thr-Dab-Dab-(Dab-Leu-Leu-Dab-Dab-Thr). [0004] Colistin is a polymyxin antibiotic produced by a specific strain of Bacillus polymyxa var.colistinus. It is an antibiotic against Gram-negative bacilli and has a bactericidal effect. It has a strong antibacterial effect on most Gram-negative bacilli. The effect of Pseudomonas aeruginosa is more significant, and it also has a good effect on Escherichia coli, Salmonella, Shigella, influenza bacillus, pertussis bacillus, aerogenes and pneumonia bacillus. Clinically, it is mainly used to treat Gram-negative bacterial infection...

Claims

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Application Information

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IPC IPC(8): C07K7/62C07K1/10C07K1/06C07K1/04C07K1/20
Inventor 宓鹏程
Owner HYBIO PHARMA
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