874340-08-6Relevant articles and documents
Preparation method of linezolid intermediate
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Paragraph 0033-0085, (2021/03/11)
The invention discloses a preparation method of a linezolid intermediate. The preparation method comprises the following steps: by taking 3-fluoro-4- (4-morpholinyl) -aniline and 2- ((S) -3-chloro-2-hydroxypropyl) isoindoline-1, 3-diketone as main raw materials, carrying out substitution reaction in an amide dipole solvent at the temperature of 90-150 DEG C to obtain N- (3-phthalimido-2- (S) -hydroxypropyl) -3-fluoro-4- (morpholinyl) aniline which is an important intermediate for synthesizing the antibiotic linezolid. The preparation steps of the intermediate are simple, dangerous reagents such as butyl lithium, sodium azide, chloroformate and methylsulfonyl chloride which are inflammable, explosive and highly toxic in the conventional process are not used in the preparation process, and the safety is high; the main raw materials of 3-fluoro-4- (4-morpholinyl) -aniline and 2- ((S) -3-chloro-2-hydroxypropyl) isoindoline-1, 3-diketone are stable in source and low in cost, the used amidedipole solvent is easy to recycle, and the pollution to the environment can be reduced.
Linezolid related substance, and preparation method and application thereof
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Paragraph 0072-0080, (2020/09/12)
The invention belongs to the technical field of medicine synthesis, and discloses a linezolid related substance, and a preparation method and application thereof. The related substance is a compound Iwith a chemical formula of C17H24FN3O4, and the prepara
Synthesis of antibiotic linezolid analogues
Reddy, Pingili Krishna,Mukkanti,Rao, Dodda Mohan
scheme or table, p. 3479 - 3482 (2012/07/28)
Several new compounds of oxazolidinone class were designed, synthesized and their analogs were evaluated for antibacterial activity against Staphylococcus aureus, Staphylococcus citreus, Proteus vulgaris, Salmonella typhimurium and Klabsiella phenumoniae. The structures of all the compounds were confirmed by IR, 1H NMR, 13C NMR and mass spectral data.
NOVEL INTERMEDIATES FOR LINEZOLID AND RELATED COMPOUNDS
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Page/Page column 11, (2008/06/13)
The present invention provides a novel process for preparation of 5-aminomethyl substituted oxazolidinones, key intermediates for oxazolidinone antibacterials including linezolid. Thus, the key intermediate of linezolid is prepared by a) reacting N-[3-Chloro-2-(R)-hydroxypropyl]-3-fluoro-4-morpholinyI aniline with potassium phthalimide; b) subjecting N-[3-pthalimido-2-(R)-hydroxypropyl]-3-fluoro-4-(morpholinyl) aniline produced in the above step to carbonylation; and c) reacting (S)-N-[[3-[3-Fluoro-4-[4-morpholinyl]phenyl]-2-oxo-5-oxazolidiriyl] methyl]phthalimide produced in the above step with hydrazine hydrate to produce (S)-N-[[3-[3-Fluoro-4-[4-morpholinyl]phenyl]-2-oxo-5-oxazolidinyl] methyl]amine.