1345879-80-2Relevant articles and documents
New isoxazolidinone and 3,4-dehydro-β-proline derivatives as antibacterial agents and MAO-inhibitors: A complex balance between two activities
Ferrazzano, Lucia,Viola, Angelo,Lonati, Elena,Bulbarelli, Alessandra,Musumeci, Rosario,Cocuzza, Clementina,Lombardo, Marco,Tolomelli, Alessandra
, p. 906 - 919 (2016/09/28)
Among the different classes of antibiotics, oxazolidinone derivatives represent important drugs, since their unique mechanism of action overcomes commonly diffused multidrug-resistant bacteria. Anyway, the structural similarity of these molecules to monoa
A convenient synthesis of the antibacterial agent linezolid
McCarthy, James R.
supporting information, p. 6846 - 6847 (2015/11/27)
Starting with 3,4-difluorobenzoic acid (8) and (S)-epichlorohydrin (13) a convergent synthesis of linezolid (1) was developed that is attractive for large scale preparation of the drug. The synthetic strategy involves a 1+3 cycloaddition reaction between the chiral epoxide 11 (prepared from 13) and isocyanate 3 (obtained from 8) that was generated in situ by a Curtius rearrangement. The resulting Schiff base precursor of linezolid (12) crystallized from the reaction mixture and was readily converted to linezolid by an acid-catalyzed hydrolysis followed by an acetylation.
PROCESSES FOR PREPARING LINEZOLID
-
Example 18, (2011/11/13)
Processes and intermediates for preparing linezolid, and pharmaceutically acceptable salts thereof, are described herein.