发明名称 |
A NOVEL PROCESS FOR THE PREPARATION OF LINEZOLID AND RELATED COMPOUNDS |
摘要 |
The present invention provides a novel process for preparation of 5-aminomethyl substituted oxazolidinones, key intermediates for oxazolidinone antibacterials including linezolid. Thus linezolid is prepared by a) reacting 3-fluoro-4-morpholinyl aniline with R-epichlorohydrin; b) subjecting N-[3-Chloro-2-(R)-hydroxypropyl]-3-fluoro-4-morpholinyl aniline produced above to carbonylation; c) reacting (5R)-5-(chloromethyl)-3-[3-fluoro-4-(4-morpholinyl)phenyl]-2-oxazolidinone produced above with potassium phthalimide; d) reacting (S)-N-[[3-[3-Fluoro-4-[4-morpholinyl]phenyl]-2-oxo-5-oxazolidinyl]methyl]phthalimide produced above with hydrazine hydrate; and e) reacting S-N-[[3-[3-Fluoro-4-[4-morpholinyl]phenyl]-2-oxo-5-oxazolidinyl]methyl]amine produced above with acetic anhydride to produce linezolid. |
申请公布号 |
WO2005099353(A2) |
申请公布日期 |
2005.10.27 |
申请号 |
WO2004IN00105 |
申请日期 |
2004.04.19 |
申请人 |
SYMED LABS LIMITED;MOHAN RAO, DODDA;KRISHNA REDDY, PINGILI |
发明人 |
MOHAN RAO, DODDA;KRISHNA REDDY, PINGILI |
分类号 |
C07D295/135;C07D413/10;C07D417/10 |
主分类号 |
C07D295/135 |
代理机构 |
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代理人 |
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主权项 |
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地址 |
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