Abstract: | A new convenient method for the synthesis of oxazolidinone antibacterials Linezolid and Eperezolid from readily available (S)‐glyceraldehyde acetonide was developed. The key steps include reductive amination of arylamine and (S)‐glyceraldehyde acetonide in the presence of NaBH4 and 4 Å sieve, followed by hydrolysis and regioselective cyclization. © 2008 Wiley Periodicals, Inc. Heteroatom Chem 19:316–319, 2008; Published online in Wiley InterScience ( www.interscience.wiley.com ). DOI 10.1002/hc.20435 |