发明公开
EP1265908A1 PROCEDE POUR LA PREPARATION DE DERIVES 9-DEOXO-8A-AZA-(8A-ALKYL)-8A-HOMOERYTHROMYCINE A A PARTIR DE LA 9-DEOXO-9(Z)-HYDROXYIMINOERYTHROMYCINE A
有权
基本信息:
- 专利标题： PROCEDE POUR LA PREPARATION DE DERIVES 9-DEOXO-8A-AZA-(8A-ALKYL)-8A-HOMOERYTHROMYCINE A A PARTIR DE LA 9-DEOXO-9(Z)-HYDROXYIMINOERYTHROMYCINE A
- 专利标题（英）：Method for preparing 9-deoxo-8a-aza-(8a-alkyl)-8a-homoerythromycin a derivatives from 9-deoxo-9(z)-hydroxyiminoerythromycin a
- 专利标题（中）：用于生产9-脱氧-9-（Z）-9- deoxo- 8A氮杂（8A-烷基）-HOMOERYTHROMYCINE甲衍生物 - 甲HYDROXYIMINOERYTHROMYCINE
- 申请号：EP01919556.9 申请日：2001-03-23
- 公开(公告)号：EP1265908A1 公开(公告)日：2002-12-18
- 发明人： LEON, Patrick , LHERMITTE, Frédéric , ODDON, Gilles , PAUZE, Denis
- 申请人： MERIAL
- 申请人地址： 17, rue Bourgelat 69002 Lyon FR
- 专利权人： MERIAL
- 当前专利权人： MERIAL
- 当前专利权人地址： 17, rue Bourgelat 69002 Lyon FR
- 代理机构： Jacobson, Claude
- 优先权： FR0003807 20000324
- 国际公布： WO01072763 20011004
- 主分类号： C07H17/08
- IPC分类号： C07H17/08
摘要：
The invention concerns a method for preparing 9-deoxo-8a-aza-(8a-alkyl)-8a-homoerythromycin A and its 8a-alkyl derivatives from 9-deoxo-9(Z)-hydroxyiminoerythromycin A via a Beckmann stereospecific rearrangement in a reaction medium using pyridine as main solvent, leading to imidate intermediates which are not isolated from said medium and which are directly engaged in a reduction step using a sufficient amount of borohydride, after extracting the pyridine with a hydrocarbon miscible therewith and wherein said imidates are insoluble. The compound (V) can be directly N-alkylated in position-8a, using an aldehyde, without being isolated from the reduction medium.
公开/授权文献:
IPC结构图谱:
| C | 化学；冶金 |
| --C07 | 有机化学 |
| ----C07H | 糖类；及其衍生物；核苷；核苷酸；核酸 |
| ------C07H17/00 | 含有直接连在糖化物基团的杂原子上的杂环基的化合物 |
| --------C07H17/04 | .仅含有氧作为杂环原子的杂环基 |
| ----------C07H17/08 | ..含有八元或更多元的杂环，如红霉素 |