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Method for preparing aminoglycoside antibiotic

A technology for aminoglycosides and antibiotics, applied in the preparation of sugar derivatives, sugar derivatives, sugar derivatives, etc., can solve the problem of not covering the inventive concept and the like

Inactive Publication Date: 2010-06-09
CHANGZHOU FANGYUAN PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Therefore, the above-mentioned patent documents cannot cover the inventive concept of this patent

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  • Method for preparing aminoglycoside antibiotic
  • Method for preparing aminoglycoside antibiotic
  • Method for preparing aminoglycoside antibiotic

Examples

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Embodiment 1

[0129] Embodiment 1: Synthesis of 1-N-(S)-3-amino-2-hydroxypropionyl gentamicin C1a

[0130] 1) Synthesis of 3, 2', 6'-tri-N-formyl gentamycin C1a

[0131] 25 grams of gentamicin C1a (GMC1a) was dissolved with 500 mL of dimethyl sulfoxide (DMSO) under stirring, cooled to room temperature, 100 mL of dichloromethane and 32 grams of cobalt acetate tetrahydrate were added, stirred and dissolved at room temperature and complexed. Add 40 g of 2-formylmercaptothiazole in batches, and react for 1 hour under stirring. Add 500mL of 5°C cold water to the reaction solution, mix evenly, separate the liquids, add 5 grams of activated carbon to the upper layer, stir for 20 minutes and filter, and the filtrate is extracted with 1 / 10 of the volume of the filtrate with dichloromethane, and extracted twice.

[0132] The upper aqueous phase was dynamically adsorbed by an 800mL HD-2 resin (ammonium type) column, washed with water to remove DMSO, and then eluted with 0.4N ammonia water. When the p...

Embodiment 2

[0139] Example 2: Synthesis of 1-N-(S)-3-amino-2-hydroxypropionyl-3″-N-demethylgentamycin C1a

[0140] Add 20 mL of water and 100 mL of DMSO to 5 grams of 3″-N-demethylgentamycin C1a, stir to dissolve, add 10 grams of zinc acetate to dissolve, and add 8.5 grams of 2-formylmercaptothiazole in batches at room temperature to react. Reaction Add 150mL cold water to the solution, mix evenly, and filter. The filtrate is dynamically adsorbed with weakly acidic cationic resin D151, washed with water, and eluted with 0.4N ammonia water. When the pH is 9.5, it starts to be collected in sections. The same components are combined and evaporated to dryness under reduced pressure to obtain Solid 3.5 g.

[0141] The above solid was subjected to 1-N acylation reaction and purified by the method of step 2) in Example 1 to obtain 1-N-(S)-3-amino-2-hydroxypropionyl-3″-N-demethylated Qingda Mycin C1a base 1.8 g.

[0142] Take 1.5 grams of the above-mentioned solids and dissolve them in 30 mL of...

Embodiment 3

[0143] Example 3: Synthesis of 1-N-(S)-3-amino-2-hydroxypropionyl-3″-N-demethylgentamycin C1a

[0144] 8 g of 1-N-(S)-3-amino-2-hydroxypropionyl gentamicin C1a sulfate was dissolved in 100 mL of water, 10 g of sodium acetate was added, and 10 g of iodine was added dropwise (dissolved in 100 mL of dimethylformamide ), stirred and reacted at 50-70° C. for 12 hours. The reaction solution was diluted with water to 400mL, dynamically adsorbed with 100mL D151 resin, washed with water, and eluted with 0.4N ammonia water. When the pH was 9.5, it began to be collected in sections. The same components were combined and evaporated to dryness under reduced pressure. Add 50 mL of water to dissolve, purify with HD-2 (weakly acidic cationic resin) resin column (height / diameter > 10), elute with 0-0.4N ammonia water, and collect in sections. Combine the same components, concentrate to dryness, dissolve with 30mL water, add 6N H 2 SO 4 Adjust the pH to 4.5-7, add 1 gram of activated carbon ...

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Abstract

The invention discloses the use of an aminoglycoside antibiotic in the preparation of medicinal compositions for treating infection with medicament-resistant bacteria, which belongs to the technical field of aminoglycoside antibiotic application. The invention provides the use of a 1-N-acyl derivative of the aminoglycoside antibiotic having a 2'-NH2-3',4'-2-de-oxy structure in the preparation of the medicinal compositions for treating infection with medicament-resistant bacteria, the preparation of the derivative and a preparation method of a preparation.

Description

[0001] This patent application is a divisional application with the application number 200710132856.4, the application date is October 9, 2007, and the invention name is "Application of an aminoglycoside antibiotic in the preparation of a pharmaceutical composition for treating drug-resistant bacterial infection". technical field [0002] The application of an aminoglycoside antibiotic in the preparation of a pharmaceutical composition for treating drug-resistant bacterial infection belongs to the technical field of aminoglycoside antibiotic application. The present invention relates to having 2'-NH 2 1-N-acylated derivatives of aminoglycoside antibiotics with 3', 4'-dideoxy structures and their application in the preparation of pharmaceutical compositions against drug-resistant bacteria. Background technique [0003] Document 1 CN1420120A, [0004] Document 2 ZL93112412.3, [0005] Document 3 ZL01133701.X, [0006] Document 4 USP4117221, [0007] Literature 5 USP4230847...

Claims

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Application Information

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IPC IPC(8): C07H15/236C07H15/234C07H1/00A61P31/04
Inventor 刘军
Owner CHANGZHOU FANGYUAN PHARMA
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