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Method for preparing Linezolid

A technology of linezolid and carbonyldiimidazole, applied in the synthesis and purification of intermediates, and the field of preparation of linezolid, which can solve the problems of difficult to meet the requirements of medicine, complex reaction mechanism, and incomplete reaction, etc., and achieve fewer reaction steps , high yield and easy operation

Active Publication Date: 2012-06-27
吉林省博大伟业制药有限公司
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  • Abstract
  • Description
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AI Technical Summary

Problems solved by technology

[0015] The synthesis method is composed of amino ionization, nucleophilic substitution reaction, deacetylation and transesterification in the final preparation step of linezolid. The reaction mechanism is complex, the reaction of intermediates 1-7 is not completed, and the yield is low. The purity of the obtained product is poor, it is difficult to refine, and it is difficult to meet the requirements of medicine

Method used

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  • Method for preparing Linezolid
  • Method for preparing Linezolid
  • Method for preparing Linezolid

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041] 3-fluoro-4-morpholine aniline

[0042]

[0043] Dissolve 40.23 grams of 3-fluoro-4-morpholine nitrobenzene in 100 milliliters of tetrahydrofuran and 400 milliliters of methanol containing 44.28 grams of ammonium formate; % palladium carbon, the reaction system was protected with nitrogen, and the reaction was stirred for 2 hours. After the reaction is complete, the reaction liquid is filtered, and the filter cake is washed successively with 40 ml of tetrahydrofuran and 80 ml of ethyl acetate. Extract with 2×100 ml of ethyl acetate, combine the organic phases, wash with 300 ml of saturated brine; dry over anhydrous magnesium sulfate, filter out the desiccant, and evaporate to dryness to obtain 30.41 g of brown product, yield: 87%. 1 H NMR (DMSO-d 6 ,600MHz): 6.77(t,1H) 6.36(m,2H) 4.98(s,2H) 3.69(br s,4H) 2. 81(br s,4H), see figure 1 .

[0044] (S)-3-Chloro-2-acetoxyacetylpropylamide

[0045]

[0046] Suspend and dissolve 100.23 g of (S)-3-chloro-2-hydroxypro...

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Abstract

The invention provides a method for preparing Linezolid. The preparation method has the advantages of few total reaction steps of the synthetic route, high yield, mild reaction of each step of the synthesis, no need of special reagent and device, and simple operation, and is suitable for large scale industrial production. High-purity of Linezolid can be prepared by the method, and medicinal requirements can be satisfied.

Description

technical field [0001] The invention provides a method for preparing linezolid, and also provides a method for synthesizing and purifying an intermediate of the preparation method, belonging to the technical field of medicine and pharmacy. Background technique [0002] The present invention relates to linezolid (formula ) is structured as follows: [0003] . [0004] Linezolid is a new type of oxazolidinone antibacterial agent developed by Pharmacia Upjohn. It is the only antibacterial agent with a new structure that has been marketed in the past 30 years. It is mainly used clinically to treat severe diseases caused by drug-resistant Gram-positive bacteria. Infect. [0005] Gram-positive bacteria are common clinical pathogens. Due to the widespread use of antibiotics, their drug resistance is rising rapidly; the proportion of methicillin-resistant Staphylococcus, glycopeptide-resistant Enterococcus, and penicillin-resistant Streptococcus pneumoniae Rising, glycopeptid...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D263/20
Inventor 李宏武李晓东谢文博张莉王龙兴
Owner 吉林省博大伟业制药有限公司
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