发明名称 |
Process for the preparation of 9-deoxo-8a-aza-(8a-alkyl)-8a-homoerythromycin A derivatives from 9-deoxo-9 (Z)-hydroxyiminoerythromycin A |
摘要 |
The invention provides a process for the preparation of 9-deoxo-8a-aza-8a-homoerythromycin Aand 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.
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申请公布号 |
US6482931(B2) |
申请公布日期 |
2002.11.19 |
申请号 |
US20010815389 |
申请日期 |
2001.03.22 |
申请人 |
MERIAL |
发明人 |
LEON PATRICK;LHERMITTE FREDERIC;ODDON GILLES;PAUZE DENIS |
分类号 |
C07H17/08;(IPC1-7):C07H1/00 |
主分类号 |
C07H17/08 |
代理机构 |
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代理人 |
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主权项 |
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地址 |
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