A New Method for the Oxazolidinone Key Intermediate of Linezolid and its Formal Synthesis

In recent years, the incidence of increase in bacterial resistance to a number of available antimicrobial agent, such as β-lactam (penicillin) antibiotics, macrolides, quinolones and vancomycin, has become a critical issue. For instance, vancomycin, an antibiotic generally considered as the ultimate solution against serious gram-positive infections, has been found ineffective on the vancomycin-resistant enterococci (VRE). Therefore, there has been an increased need for totally new agents for effective therapy of gram-positive infections by antimicrobial-resistant species. In the search for a new antimicrobial agent, several kinds of syn-thetic organic compounds have been focused. Among these new compounds, an oxazolidinone was first suggested as a candidate for use as a new antimicrobial agent by Du Pont scientists in 1978. With several biological assay tests, it wa