L. Yun, Huang Chang-jiang
2005
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Journal
Journal of Tianjin Normal University
Abstract
Linezolid is a synthetic oxazolidinones antibacterial agent which has been marketed recently.The synthetic methods reported by literature was modified and its key intermediate(R)-N-[3-[3-fluoro-4-morpholinyl]phenyl]-2-oxo-5-oxazolidinyl]methanol(1)was successfully synthesized.With cheap triethylamine substituting for N,N-diisopropylethylamine to prepare 3-fluoro-4-morpholinylnitrobenzene,the reaction time curtailed from 72h to 6h;By using Pd/C(10%) as deoxidizer in acetone,the solution reacted with benzyl chloroformate directly to prepare N-carbobenzoxy-3-fluoro-4-morpholinylaniline,which merged two steps into one and got excellent yield(93.2%).When preparing compound(1),the temperature was raised to approximate-50 ℃,making the condition milder than that of literature.