Rina Sanzuotong Synthesis

The categories and mechanisms of action of antibacterial agents were introduced briefly in the paper. Linezolid, a new antibacterial drug, was introduced in detail, including its antibacterial mechanisms, antibacterial activity, pharmacokinetic properties and clinical utilitiy.The synthetic methods of linezolid were discussed, and a route siutable for industrial production was selected in this paper. We used 3,4-difluronitrobenzene as the starting material, via substitution, reduction, and acylation to gain the intermediate N-benzyloxycarbonyl-3-fluoro-4-morpholinoaniline. (S)-N-[2-(acetyloxy)-3-chloropropyl]a-cetamide was prepared from S-epichlorohydrin via amination and acetylation. In the presence of lithium tert-butoxide and methanol, N-benzyloxycarbonyl-3-fluoro-4-(4-morpho-lino)aniline reacted with (S)-N-[2-(acetyloxy)-3-chloropropyl]acetamide to give linezolid in total yield of 70.9%(from 3,4-difluronitrobenzene).The structure of linezolid was confiemed by IR,1-NMR, 13C-NMR and MS.