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A short synthesis of oxazolidinone derivatives linezolid and eperezolid: A new class of antibacterials

✍ Scribed by Braj B. Lohray; Sundarababu Baskaran; B. Srinivasa Rao; B. Yadi Reddy; I. Nageswara Rao


Book ID
104261676
Publisher
Elsevier Science
Year
1999
Tongue
French
Weight
100 KB
Volume
40
Category
Article
ISSN
0040-4039

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Starting from the D-mannitol derivative (I), a straightforward synthesis of the chiral oxazolidines (VII) including precursors (VIIb) and (VIIc) of linezolid and eperezolid is detailed. Furthermore, the azide (VIIb) is converted to linezolid (IX) with thioacetic acid.

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## 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 NaBH~4~ an