A kind of purification method of telavancin

A technology of telavancin and purification methods, applied in peptide preparation methods, chemical instruments and methods, organic chemistry, etc., can solve problems such as insufficient purity

Active Publication Date: 2021-05-07
FUJIAN INST OF MICROBIOLOGY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0005] In order to solve the technical problem of insufficient purity in the method for preparing telavancin, the present invention provides a purification method of telavancin, specifically the present invention is achieved in this way:

Method used

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  • A kind of purification method of telavancin
  • A kind of purification method of telavancin
  • A kind of purification method of telavancin

Examples

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Effect test

Embodiment 1

[0038] A method for purifying telavancin, comprising the steps of:

[0039] 1) Mix the crude product mixture containing telavancin with methanol-formic acid-water solution in a weight ratio of 1:5, dissolve the crude product mixture, filter out solid insolubles, and obtain a filtrate; the above-mentioned methanol-formic acid-water solution is in a volume ratio of 2:1 : 1 is configured; the crude product mixture of telavancin in the described step 1) is vancomycin hydrochloride and N-(9-fluorenylmethoxycarbonyl)-decylaminoacetaldehyde occurs reductive amination reaction, and then The crude telavancin synthesized by removing the 9-fluorenylmethoxycarbonyl protecting group and carrying out Mannich reaction with aminomethylphosphonic acid;

[0040] 2) Pass the filtrate through the well-balanced chromatographic medium of the eluent, the weight ratio of the loading filtrate to the chromatographic medium is 1:50; the chromatographic medium is naphthyl bonded silica gel; the eluent is...

Embodiment 2

[0046] A method for purifying telavancin, comprising the steps of:

[0047] 1) Mix the crude product mixture containing telavancin with methanol-formic acid-water solution in a weight ratio of 1:10, dissolve the crude product mixture, filter out solid insolubles, and obtain a filtrate; the above-mentioned methanol-formic acid-water solution is in a volume ratio of 2:1 : 1 is configured; the crude product mixture of telavancin in the described step 1) is a sample with a purity of more than 95% through one purification;

[0048] 2) Pass the filtrate through the well-balanced chromatographic medium of the eluent, the weight ratio of the loading filtrate to the chromatographic medium is 1:100; the chromatographic medium is pyrenyl ethyl bonded silica gel; the eluent is 5 column volumes The solvent A-phosphate buffer solution, the phosphate buffer solution is: diammonium hydrogen phosphate 0.05mol / L, the buffer solution with phosphoric acid to adjust the pH at 2.5: when solvent A i...

Embodiment 3

[0054] A method for purifying telavancin, comprising the steps of:

[0055] 1) Mix the crude product mixture containing telavancin with methanol-formic acid-water solution in a weight ratio of 1:6, dissolve the crude product mixture, filter out solid insolubles, and obtain a filtrate; the above-mentioned methanol-formic acid-water solution is in a volume ratio of 2:1 : 1 is configured; the crude product mixture of telavancin in the step 1) is or a sample with a purity of more than 95% through a purification;

[0056] 2) Pass the filtrate through the well-balanced chromatographic medium of the eluent, the weight ratio of the loading filtrate to the chromatographic medium is 1:80; the chromatographic medium is pyrenyl ethyl bonded silica gel; the eluent is 4 column volumes The solvent A-phosphate buffer solution, the phosphate buffer solution is: diammonium hydrogen phosphate 0.03mol / L, the buffer solution with phosphoric acid to adjust the pH at 2.3: when the solvent A is ethan...

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Abstract

The present invention provides a method for purifying telavancin, which comprises the following steps: 1) mixing and dissolving the crude product mixture containing telavancin with methanol-formic acid-water solution according to the weight ratio of 1:5 to 1:10; 2) mixing and dissolving The filtrate is purified by a well-balanced chromatographic medium of the eluent; 3) Concentrate the above-mentioned chromatographic solution through a nanofiltration membrane and supplement an aqueous hydrochloric acid solution with a pH of 4-5 to obtain a concentrated solution of hydrochloric acid; 4) Heat the above-mentioned concentrated solution to 40°C to 60°C, mixed with a solvent B of acetonitrile, methanol, ethanol, acetone; 5) mixed with a solvent C of diethyl ether or methyl tert-butyl ether, stirred and cooled to 4°C to 10°C, filtered to obtain Tetrahydrochloride The solid of ten thousand stars. The chromatographic medium selected in this case is naphthyl bonded silica gel or pyrenylethyl bonded silica gel, combined with an appropriate acid solution or salt solvent system, the telavancin compound has a closer effect on the performance of the material medium during the separation process, and can be separated to obtain High purity telavancin hydrochloride.

Description

technical field [0001] The invention relates to the field of antibiotic drugs, in particular to a method for purifying telavancin. Background technique [0002] Telavancin is the first semi-synthetic novel glycolipopeptide antibiotic, with its unique mechanism of action and good clinical therapeutic effect, the market prospect is very broad. Telavancin has higher activity against MRSA and MRSE than vancomycin and teicoplanin, and its half-life is longer than that of vancomycin. Clinically, it can be administered once a day. The half-life of dalgivancin is as long as 174h, clinically it can be administered once a week. Oritavancin has very prominent pharmacodynamic properties, its half-life is 393 hours, and it can be administered once in each course of treatment. [0003] At present, the research on the synthesis process of telavancin mainly focuses on the synthesis of hydrophobic side chain N-(9-fluorenylmethoxycarboxy)-decyl amino acid by different methods. Telavancin w...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07K9/00C07K1/20C07K1/16C07K1/34C07K1/14
CPCY02P20/55
Inventor 乐占线黄楷庄鸿陈秀明陈宏江红连云阳乐雨银
Owner FUJIAN INST OF MICROBIOLOGY
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