Prepn process of (R)-N-(3-fluoro-4-morpholinyl phenyl)-oxazolone-5-methyl alcohol

A technology of morpholine phenyl and preparation process is applied in the field of new synthesis process of important intermediate-N-oxazolone-5-methyl alcohol, and can solve the problem of rare raw materials, long process route and high price of the original process problem, to achieve the effect of simple process, low price and mild reaction
CN1772750AInactive Publication Date: 2006-05-17ZHENGZHOU UNIV
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
ZHENGZHOU UNIV
Publication Date
2006-05-17
Estimated Expiration
Not applicable · inactive patent

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Abstract

The present invention discloses the preparation process of Linezolid, and the preparation process includes the following steps: condensation of morpholine and 3, 4-difluoro nitrobenzene; reduction into 3-fluoro-4-morpholinyl aniline under the catalysis of Fe, and acylation with phosgene into 3-fluoro-4-morpholinylphenyl isocyanate; cyclization with (R)-butyl glycidate to produce (R)-N-(3-fluoro-4-morpholinylphenyl)-oxazolone-5-methyl alcohol; and further conventional synthesis steps. The present invention has simple technological process, mild reaction condition, cheap catalyst and low production cost, and is favorable to industrial production.
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Description

(1) Technical field

[0001] The present invention relates to a new process for the preparation of pharmaceutical intermediates, specifically an important intermediate (R)-N-(3-fluoro-4-morpholine phenyl)-oxazolone-5 involved in the synthesis of antibacterial drug Linezolid - A new process for the synthesis of methyl alcohol. (2) Background technology

[0002] (R)-N-(3-fluoro-4-morpholine phenyl)-oxazolone-5-methyl alcohol (hereinafter referred to as oxazolone) is a new generation of antibacterial drugs (R)-N-(3 -Fluoro-4-morpholine phenyl)-2-oxo-oxazole-5-methyl-acetamide (hereinafter referred to as Linezolid or Linezolid) is an important intermediate involved in the synthesis process.

[0003] Linezolid is a newest fully synthetic chemical antibacterial drug with the chemical name (R)-N-(3-fluoro-4-morpholine phenyl)-2-oxo-oxazole-5-methyl-acetamide. It was first successfully developed by pharmacia∝Upjohn in the 1990s and approved for marketing in the United States in 2000...

Claims

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