A convenient synthesis of linezolid through Buchwald-Hartwig amination. (31st August 2022)

• Record Type: Journal Article
• Authors: Wang, Keyin; Chen, Yinzhe; Wang, Siyuan; Zhang, Qian
• Is Part Of: Tetrahedron letters. Volume 105(2022)
• Publication Date: 2022-08-31
• Subjects: BMGQMLDNAYSSOT-ZNZWXRCUSA-N -- NKYJEIUMGFRATE-YGBVEIAUSA-N -- OWGUMPFGBPKPRD-CNXQYKSLSA-N; Antibiotic -- Gram-positive bacteria -- Linezolid -- Buchwald-Hartwig reaction -- Synthesis of new oxazolidinones; Chemistry, Organic -- Periodicals; 547.005
• DOI: 10.1016/j.tetlet.2022.154050
• Languages: English
• ISSNs: 0040-4039

Abstract

Graphical abstract: Abstract: 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.