Raghu Mitra Alla;Aruna Kumari Sirigiri;Naga Kama Kumar Mareedu;Ajay Kumar Dubey
发明人:
Raghu Mitra Alla,Ajay Kumar Dubey,Aruna Kumari Sirigiri,Naga Kama Kumar Mareedu
申请号：
US13820568
公开号：
US09376407B2
申请日:
2012.02.21
申请国别(地区):
US
年份:
2016
代理人:
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.
