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Synthetic method of antimicrobial medicament

A synthesis method and technology of antibacterial drugs, applied in the field of synthesis of antibacterial drugs, can solve problems such as harsh synthesis conditions and unfavorable industrial production, and achieve the effect of simple synthesis steps and low requirements for synthesis conditions

Inactive Publication Date: 2012-05-16
张芮
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] The synthesis of linezolid has been reported, but in the synthesis process, sensitive reagents such as BuLi, -78 ° C, nitrogen protection and harsh synthesis conditions are always used, which is not conducive to industrial production

Method used

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  • Synthetic method of antimicrobial medicament
  • Synthetic method of antimicrobial medicament
  • Synthetic method of antimicrobial medicament

Examples

Experimental program
Comparison scheme
Effect test

Embodiment Construction

[0024] The synthetic steps of the present invention are:

[0025] 1.3 Synthesis of m-fluorophenyl 2-oxo-5-oxazolidinyl chloride

[0026] The reaction equation is:

[0027]

[0028] 2.3 Synthesis of m-fluorophenyl 2 oxo 5 oxazolidine azidomethane

[0029] The reaction equation is:

[0030]

[0031] 3.3 Synthesis of m-fluorophenyl 2-oxo-5-oxazolidinylmethylacetamide

[0032] The reaction equation is:

[0033]

[0034] 4.3 Synthesis of (3' fluoro 4' bromo) phenyl 2 oxo 5 oxazolidinylmethylacetamide

[0035] The reaction equation is:

[0036]

[0037] 5. Synthesis of linezolid

[0038] The reaction equation is:

[0039]

[0040] The drug intermediate and final product of the present invention have been confirmed by NMR and mass spectrograms.

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Abstract

A synthetic method of an antimicrobial medicament belongs to the field of medicament processing and specifically relates to a synthetic method of an antimicrobial medicament. The invention provides a simple and safe synthetic method of an antimicrobial medicament. The method of the invention comprises steps of: synthesis of 3-m fluorophenyl-2-oxo-5-oxazolidinyl methyl chloride; synthesis of 3-m fluorophenyl-2-oxo-5-oxazolidin diazomethane; synthesis of 3-m fluorophenyl-2-oxo-5-oxazolidin methylacetamide; synthesis of 3(3'-fluorine-4'-bromine) phenyl-2-oxo-5- oxazolidin methylacetamide; and synthesis of linezolid.

Description

Technical field: [0001] The invention belongs to the field of medicine processing, and more specifically relates to a synthesis method of antibacterial medicine. Background technique: [0002] Linezolid is a fully chemically synthesized antibacterial drug that was officially approved by the US FDA in April 2000 for the treatment of bacteremia caused by vancomycin-resistant Enterococci and pneumonia caused by methicillin-resistant Staphylococcus aureus and treatment of combined skin infections and bacteremia caused by penicillin-resistant Streptococcus pneumoniae. Due to its unique mechanism of action and no cross-resistance with other antibacterial drugs, it has attracted much attention. [0003] The synthesis of linezolid has been reported, but in the synthesis process, sensitive reagents such as BuLi, -78°C, nitrogen protection and harsh synthesis conditions are always used, which is not conducive to industrial production. Invention content: [0004] The present invent...

Claims

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Application Information

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IPC IPC(8): C07D263/20
Inventor 张芮
Owner 张芮
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