Method for purifying telavancin

A technology of telavancin and purification method, which can be used in the preparation methods of peptides, chemical instruments and methods, organic chemistry, etc., and can solve problems such as insufficient purity

Active Publication Date: 2018-01-26
FUJIAN INST OF MICROBIOLOGY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0006] In order to solve the technical problem of insufficient purity in the method for preparing telavancin, the p...

Method used

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  • Method for purifying telavancin
  • Method for purifying telavancin
  • Method for purifying telavancin

Examples

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Embodiment 1

[0036] A method for purifying telavancin, comprising the steps of:

[0037] 1) Mix the reaction mixture containing telavancin with methanol-formic acid-water solution in a weight ratio of 1:5, dissolve the reaction mixture, filter out solid insolubles, and obtain the filtrate; the above-mentioned methanol-formic acid-water solution is in a volume ratio of 2: 1:1 configuration; the reaction mixture of telavancin is a reductive amination reaction between vancomycin hydrochloride and N-(9-fluorenylmethoxycarbonyl)-decylaminoacetaldehyde, and then removes 9- Telavancin crude product synthesized by Mannich reaction with fluorenylmethoxycarbonyl protecting group and aminomethylphosphonic acid;

[0038] 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 octadecyl bonded silica gel; the eluent is 3 column volumes The solvent A-phosphate buffer ...

Embodiment 2

[0041] A method for purifying telavancin, comprising the steps of:

[0042] 1) Mix the reaction mixture containing telavancin with methanol-formic acid-water solution in a weight ratio of 1:10, dissolve the reaction mixture, filter out solid insolubles, and obtain the filtrate; the above-mentioned methanol-formic acid-water solution is in a volume ratio of 2: 1:1 configuration; the reaction mixture of telavancin is a reductive amination reaction between vancomycin hydrochloride and N-(9-fluorenylmethoxycarbonyl)-decylaminoacetaldehyde, and then removes 9- Telavancin crude product synthesized by Mannich reaction with fluorenylmethoxycarbonyl protecting group and aminomethylphosphonic acid;

[0043] 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 octadecyl bonded silica gel; the eluent is 5 column volumes The solvent A-phosphate buf...

Embodiment 3

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

[0047] 1) Mix the reaction mixture containing telavancin with methanol-formic acid-water solution in a weight ratio of 1:7, dissolve the reaction mixture, filter out solid insolubles, and obtain the filtrate; the above-mentioned methanol-formic acid-water solution is in a volume ratio of 2: 1:1 configuration; the reaction mixture of telavancin is a reductive amination reaction between vancomycin hydrochloride and N-(9-fluorenylmethoxycarbonyl)-decylaminoacetaldehyde, and then removes 9- Telavancin crude product synthesized by Mannich reaction with fluorenylmethoxycarbonyl protecting group and aminomethylphosphonic acid;

[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 1:70; the chromatographic medium is octadecyl bonded silica gel; the eluent is 4 column volumes The solvent A-phosphate buffe...

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Abstract

The invention provides a method for purifying telavancin. The method comprises the following steps: 1) a reaction mixture contain telavancin is mixed and dissolved by a methanol-formic acid-aqueous solution according to weight ratio being 1: 5 to 1: 10; 2) a filtrate is purified by a chromatography media balanced by an eluate, and the weight ratio of a sample filtrate to the chromatography media is 1: 50 to 1: 100; the chromatography media is octadecyl silane; and 3) the above chromatography liquid is concentrated through a nanofiltration membrane to more than 1/10 original volume, a hydrochloric acid aqueous solution with a pH value being 4-5 is supplemented when the chromatography liquid is concentrated to 1/5 original volume during the above process, buffer salt is removed after repetition is carried out for 3-5 times, and hydrochloric acid is added for adjusting the pH value to 0.5-2 to obtain a concentrate. The selected chromatography media octadecyl silane combines a proper acidsolution or a salt solvent system for separating the high-purity hydrochloric acid telavancin during a separating process of a telavancin compound due to tight performance effect with a material medium.

Description

technical field [0001] The invention relates to the field of antibiotic drugs, in particular to a method for purifying telavancin. Background technique [0002] Glycopeptide Antibiotics, properties: Glycopeptide antibiotics have a highly modified polypeptide backbone in structure, and the target is on the bacterial cell wall component D-alanyl-D-alanine, usually through It specifically binds to the peptidoglycan precursor small peptide with D-Ala-D-Ala as the terminal on the bacterial cell wall, inhibits the elongation or / and cross-linking of the peptidoglycan on the bacterial cell wall, thereby inhibiting the synthesis of the cell wall and eventually leading to bacterial cell death .. According to the different amino acids contained, it can be divided into four families: vancomycin family, ristocetin family, avoparcin family, and symmonicin family. The first generation of glycopeptide antibiotics includes vancomycin, norvancomycin, and teicoplanin, which are directly deri...

Claims

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Application Information

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IPC IPC(8): C07K9/00C07K1/20C07K1/16C07K1/14C07K1/34
CPCY02P20/55
Inventor 黄楷乐占线庄鸿陈秀明江红陈宏连云阳乐雨银
Owner FUJIAN INST OF MICROBIOLOGY
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