Processes for the preparation of linezolid intermediate
    58.
    发明申请
    Processes for the preparation of linezolid intermediate 审中-公开
    制备利奈唑胺中间体的方法

    公开(公告)号:US20080045707A1

    公开(公告)日:2008-02-21

    申请号:US11977344

    申请日:2007-10-23

    IPC分类号: C07D413/10

    摘要: The present invention provides improved methods of converting R—N-(4-morpholiyl-3-fluorophenyl)-2-oxo-5-oxazolidinyl-methyl azide (III) to the intermediate S—N-(4-morpholinyl-3-fluorophenyl)-2-oxo-5-oxazolidinyl-methyl amine (II) that involve the production of fewer by-products than previous methods. The amine (II) may then be converted into linezolid (I) of high chemical purity with respect to the inactive R-enantiomer and bis-linezolid (IV), and is in high yield, without the need for tedious, complicated purification steps, such as chromatography.

    摘要翻译: 本发明提供了将RN-(4-吗啉基-3-氟苯基)-2-氧代-5-恶唑烷基 - 甲基叠氮化物(III)转化成中间体SN-(4-吗啉基-3-氟苯基)-2- 涉及与先前方法相比产生较少副产物的5-氧代-5-恶唑烷基甲基胺(II)。 然后可以将胺(II)相对于无活性R-对映异构体和双利奈唑胺(IV)转化为高化学纯度的利奈唑胺(I),并且产率高,无需繁琐,复杂的纯化步骤, 如色谱。