A kind of preparation method of linezolid

A technology of linezolid and the next step, which is applied in the field of linezolid preparation to achieve the effect of saving purification steps and reducing dosage

Inactive Publication Date: 2011-12-07
SHANDONG LUKANG PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Up to now, in the prior art, there is no effective method for preparing linezolid with...

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  • A kind of preparation method of linezolid
  • A kind of preparation method of linezolid
  • A kind of preparation method of linezolid

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Embodiment Construction

[0024] Unless otherwise stated, all reactions were performed in flame-dried or oven-dried glassware under a dry nitrogen atmosphere with magnetic stirring. Sensitive liquids and solutions are added to reaction vessels by injection or catheters through rubber stoppers.

[0025] All temperatures reported are in uncorrected degrees Celsius (°C). All parts and percentages are by weight unless otherwise indicated.

[0026] Commercially available reagents and solvents were used without secondary purification.

[0027] Thin-layer chromatography (TLC) was performed using prefabricated Whatman silica gel 60A GF254 thin-layer glass plates (250 μm). One or more of the following techniques can be used for TLC inspection: 1) ultraviolet irradiation, 2) placing in iodine vapor, 3) spraying with 10% phosphomolybdic acid ethanol solution, heating to develop color, 4) spraying with cerium sulfate solution, Heating color.

[0028] Column chromatography used 230-400 mesh EM Science silica ge...

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PUM

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Abstract

The invention discloses a preparation method of linezolid. The method comprises reacting 3,4-difluoronitrobenzene to generate 3-fluoro-4-morpholine nitrobenzene, and then adding a small amount of catalyst Pd/C, In the case of hydrogen, 3-fluoro-4-morpholine aniline is obtained, which does not undergo separation and purification on a silica gel column, and reacts to generate N-Cbz-3-fluoro-4-morpholine aniline, and then reacts with the intermediate 3-chloro- 2-Acetoxyacetylpropylamide reacts to form linezolid. The preparation method of the invention not only reduces numerous purification steps in the reaction, but also reduces the amount of catalyst used, thereby making the preparation of linezolid more effective and more environmentally friendly.

Description

technical field [0001] The invention relates to a preparation method of linezolid. The invention also includes the preparation and purification of related compounds and intermediates. Background technique [0002] Linezolid is an inhibitor of bacterial protein synthesis. Unlike other antibacterial drugs, linezolid does not affect peptidyl transferase activity, but selectively binds to the 50S subunit ribosome, interfering with the formation of the 70S initiation complex including mRNA, 30S ribosomes and initiation factors, thereby inhibiting bacterial protein synthesis. Because linezolid has a unique site and mode of action and acts on the initial stage of protein translation, it is not easy to cross-resistance with other antibacterial drugs that inhibit bacterial protein synthesis. It is also not easy to develop drug resistance in vitro. [0003] Linezolid is a synthetic oxazolidinone antibiotic approved by the US FDA in 2000 for the treatment of infections caused by Gr...

Claims

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Application Information

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IPC IPC(8): C07D263/20
Inventor 张淑婷郝岩宋爱刚范震单光举吕桂奎赵永徐荔黄伟强孔维苓
Owner SHANDONG LUKANG PHARMA
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