发明授权
- 专利标题: Process for preparation of Linezolid and its novel intermediates
- 专利标题(中): 利奈唑胺及其新型中间体的制备方法
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申请号: US13820568申请日: 2012-02-21
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公开(公告)号: US09376407B2公开(公告)日: 2016-06-28
- 发明人: Raghu Mitra Alla , Ajay Kumar Dubey , Aruna Kumari Sirigiri , Naga Kama Kumar Mareedu
- 申请人: Raghu Mitra Alla , Ajay Kumar Dubey , Aruna Kumari Sirigiri , Naga Kama Kumar Mareedu
- 申请人地址: IN Moosapet, Balanagar, Hyderabad
- 专利权人: Lee Pharma Limited
- 当前专利权人: Lee Pharma Limited
- 当前专利权人地址: IN Moosapet, Balanagar, Hyderabad
- 代理机构: Davidson, Davidson & Kappel LLC
- 优先权: IN2451/CHE/2010 20110224
- 国际申请: PCT/IN2012/000121 WO 20120221
- 国际公布: WO2012/114355 WO 20120830
- 主分类号: C07D263/06
- IPC分类号: C07D263/06 ; C07D263/20 ; C07D263/14 ; C07D265/30 ; C07D269/00 ; C07D413/10 ; A61K31/5377
摘要:
A novel process for preparing oxazolidinone antibacterial agent Linezolid including key intermediates of oxazolidinones comprising: reacting 3-fluoro-4-morpholinyl aniline with R-epichlorohydrin; carbonylation to form oxazolidinone derivative; acetylation of (5R)-5-(chloromethyl)-3-(3-fluoro-4-morpholinophenyl-oxazolidin-2-one with sodium acetate to get novel intermediate; hydrolysis of (R)-3-(3-fluoro-4-morpholinophenyl)-2-oxo-5-oxazolidinyl methyl acetate; mesylation of (R)-3-(3-fluoro-4-morpholinophenyl)-2-oxo-5-oxazolidinyl methanol; reaction of (R)-3-(3-fluoro-4-morpholinophenyl)-2-oxo-5-oxazolidinyl methyl methane sulphonate with potassium phthalimide; hydrolysis of (S)-3-(3-fluoro-4-morpholinophenyl)-2-oxo-5-oxazolidinyl methyl phthalimide with hydrazine hydrate; acetylation of (S)-3-(3-fluoro-4-morpholinophenyl)-2-oxo-5-oxazolidinyl methyl amine with acetic anhydride yields Linezolid in high yield.
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