Aminoglycoside antibiotics

A technology of aminoglycosides and antibiotics, applied in the direction of amino sugar, etc., can solve the problem of not being able to cover the invention concept

Inactive Publication Date: 2008-03-12
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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Examples

Experimental program
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Embodiment 1

[0127] Example 1: Synthesis of 1-N-(S)-3-amino-2-hydroxypropionyl gentamicin C1a 1) 3,2 ', 6'-three-N-formyl gentamicin C1a synthesis

[0128] 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 and mix evenly, separate the liquids, add 5 grams of activated carbon to the upper layer and stir for 20 minutes to filter, and the filtrate is extracted with 1 / 10 of the volume of the filtrate with dichloromethane, and extracted twice.

[0129] 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 pH reache...

Embodiment 2

[0136] Example 2: Synthesis of 1-N-(S)-3-amino-2-hydroxypropionyl-3″-N-demethylgentamycin C1a

[0137] 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.

[0138] 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.

[0139] Take 1.5 grams of the above-mentioned solids and dissolve them in 30 mL of...

Embodiment 3

[0140] Example 3: Synthesis of 1-N-(S)-3-amino-2-hydroxypropionyl-3″-N-demethylgentamycin C1a

[0141] 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 present invention relate4s to an aminoglycoside antibiotic which belongs to the application technology filed of aminoglycoside antibiotic. The present invention provides the derivative of the structure of 2'-NH 2 -3 ', 4'-deoxy-3'-N demethylase 1-N acylation as well as the application of the derivative in the preparation of medicinal combination in the treatment of drug-resistant virus infections.

Description

technical field [0001] An aminoglycoside antibiotic belongs to the technical field of aminoglycoside antibiotic application. The present invention provides with 2'-NH 2 -3′, 4′-dideoxy-3″-N demethylated-1-N acylated derivatives. Background technique [0002] Document 1 CN1420120A, [0003] Document 2 ZL93112412.3, [0004] Document 3 ZL01133701.X, [0005] Document 4 USP4117221, [0006] Literature 5 USP4230847, [0007] Document 6 USP5442047. [0008] Since the listing of aminoglycoside antibiotics, their broad-spectrum antibacterial activity, especially against Gram-negative bacteria, has a good synergistic effect with β-lactam antibiotics widely used in clinical practice and their main otic , Renal toxicity is predictable, thus becoming an indispensable class of antibiotics in clinical practice. [0009] In order to reduce toxicity and enhance the activity against drug-resistant bacteria, some semi-synthetic aminoglycoside antibiotics have also been developed, suc...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07H5/06
Inventor 刘军
Owner CHANGZHOU FANGYUAN PHARMA
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