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    Process for the preparation of 9-deoxo-8a-aza-(8a-alkyl)-8a-homoerythromycin A derivatives from 9-deoxo-9 (Z)-hydroxyiminoerythromycin A
    5.
    发明授权
    Process for the preparation of 9-deoxo-8a-aza-(8a-alkyl)-8a-homoerythromycin A derivatives from 9-deoxo-9 (Z)-hydroxyiminoerythromycin A 有权
    9-脱氧-9（Z） - 羟基亚氨基红霉素A的9-脱氧-8a-氮杂 - （8a-烷基）-8a-高红霉素A衍生物的制备方法

    公开(公告)号：US06482931B2

    公开(公告)日：2002-11-19

    申请号：US09815389

    申请日：2001-03-22

    申请人： Patrick Leon ,  Frederic Lhermitte ,  Gilles Oddon ,  Denis Pauze

    发明人： Patrick Leon ,  Frederic Lhermitte ,  Gilles Oddon ,  Denis Pauze

    IPC分类号： C07H100

    CPC分类号： C07H17/08

    摘要： The invention provides a process for the preparation of 9-deoxo-8a-aza-8a-homoerythromycin A and of its 8a-alkylated derivatives from 9-deoxo-9(Z)-hydroxyiminoerythromycin A via a stereospecific Beckmann rearrangement in a reaction mixture using pyridine as main solvent, resulting in imidate intermediates which are not isolated from said mixture and which are employed directly in a reduction stage using a sufficient amount of borohydride, after extraction of the pyridine with a hydrocarbon which is miscible with the latter and in which said imidates are insoluble. The compound V can be directly N-alkylated at the 8a-position using an aldehyde without being isolated from the reduction mixture.

    摘要翻译： 本发明提供了在反应混合物中使用吡啶，通过立体特异性Beckmann重排从9-脱氧-9（Z） - 羟基亚氨基红霉素A制备9-脱氧-8a-氮杂-8a-高红霉素A及其8-烷基化衍生物的方法 作为主要溶剂，得到亚胺化中间体，其不从所述混合物中分离，并且在用与后者可混溶的烃萃取吡啶后，使用足够量的硼氢化物直接用于还原阶段，并且其中所述亚胺酯 是不溶的。 化合物V可以使用醛直接在8a位进行N-烷基化，而不从还原混合物中分离。