A convenient synthesis of linezolid through Buchwald-Hartwig amination

A new method was developed for the synthesis of Linezolid from commercially available (R)-3-(4-bromo-3-fluorophenyl)-5-(hydroxymethyl)oxazolidin-2-one. Linezolid is an antibiotic belongs to the family of oxazolidinones, it is successfully synthesized through a new method which include Buchwald-Hartwig amination reaction and Gabriel amine synthesis as the key steps. The synthetic route is easy to perform and with high yield. This new method provides a huge possibility for the synthesis of new linezolid derivatives that may possibly tackle the problem of bacteria resistance to oxazolidinones.