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Preparation method for Linezolid

A kind of technology of linezolid and linazolid, applied in the field of preparation of linezolid

Inactive Publication Date: 2013-11-06
济南德爱医药技术有限公司
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Problems solved by technology

However, the Cbz-protected compound used by the author is obtained through three-step synthesis and purification, and the amount of catalyst Pd / C is 10%, and the time required for hydrogenation reduction is as long as 6 hours

Method used

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  • Preparation method for Linezolid
  • Preparation method for Linezolid
  • Preparation method for Linezolid

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Embodiment Construction

[0033] 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. All temperatures reported are in uncorrected degrees Celsius (°C). All parts and percentages are by weight unless otherwise indicated. Commercially available reagents and solvents were used without secondary purification.

[0034] 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 for color development, 4) spraying with cerium sulfate solution, Heating color. For column chromatography, 230-400 mesh EM Science silica gel G was used.

[0035] ...

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Abstract

The invention relates to a preparation method for Linezolid. Compared with the reported preparation method for the Linezolid, the preparation method has the advantages that: supercritical carbon dioxide serves as a solvent during hydrogenation reduction, so that the using amount of a catalyst and the use of the traditional solvent can be reduced; in addition, purification of an intermediate and the final product is improved, so that the method is effective and environment-friendly and the yield of the Linezolid can reach 82 weight percent.

Description

technical field [0001] The invention relates to a preparation method of linezolid, including the preparation and purification methods 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 50S subunit ribosomes, interfering with the formation of 70S initiation complexes 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 have 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 Gram-positive...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D263/20
CPCY02P20/54
Inventor 郝岩
Owner 济南德爱医药技术有限公司
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