4.4 Article

A convenient synthesis of linezolid through Buchwald-Hartwig amination

Journal

TETRAHEDRON LETTERS
Volume 105, Issue -, Pages -

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.tetlet.2022.154050

Keywords

Antibiotic; Gram-positive bacteria; Linezolid; Buchwald-Hartwig reaction; Synthesis of new oxazolidinones

Funding

  1. Research Development Fund [RDF- 20-02-30]
  2. Xian Jiaotong-Liverpool University [RDF- 20-02-30]
  3. [PGRS2112027]

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A new method for synthesizing Linezolid, an antibiotic belonging to the family of oxazolidinones, was developed. The method involves Buchwald-Hartwig amination reaction and Gabriel amine synthesis as key steps and has shown high efficiency and easy operation. This new method opens up possibilities for synthesizing new Linezolid derivatives that may help address bacteria resistance to oxazolidinones.
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.(c) 2022 Elsevier Ltd. All rights reserved.

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