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    • 10. 发明申请
    • NOVEL INTERMEDIATES FOR LINEZOLID AND RELATED COMPOUNDS
    • 线性相关化合物的新型中间体
    • WO2006008754A1
    • 2006-01-26
    • PCT/IN2004/000218
    • 2004-07-20
    • SYMED LABS LIMITEDMOHAN RAO, DoddaKRISHNA REDDY, Pingili
    • MOHAN RAO, DoddaKRISHNA REDDY, Pingili
    • C07D263/24
    • C07D209/48C07D263/20
    • The present invention provides a novel process for preparation of 5­aminomethyl 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.
    • 本发明提供了一种制备5氨基甲基取代的恶唑烷酮的新方法,包括利奈唑胺的恶唑烷酮抗菌剂的关键中间体。 因此,利奈唑胺的关键中间体通过以下步骤制备:a)使N- [3-氯-2-(R) - 羟丙基] -3-氟-4-吗啉代苯胺与邻苯二甲酰亚胺反应; b)将上述步骤中生产的N- [3-苯基亚氨基-2-(R) - 羟丙基] -3-氟-4-(吗啉基)苯胺进行羰基化; 和c)使上述步骤中制备的(S)-N - [[3- [3-氟-4- [4-吗啉基]苯基] -2-氧代-5-恶唑烷基]甲基]邻苯二甲酰亚胺与水合肼反应, (S)-N - [[3- [3-氟-4- [4-吗啉基]苯基] -2-氧代-5-恶唑烷基]甲基]胺。