PROCESS FOR PRODUCTION OF LIPID A ANALOGUE
    1.
    发明公开
    PROCESS FOR PRODUCTION OF LIPID A ANALOGUE 审中-公开
    VERFAHREN ZUR HERSTELLUNG EINES LIPID-A-ANALOGONS

    公开(公告)号:EP1939209A1

    公开(公告)日:2008-07-02

    申请号:EP06796921.2

    申请日:2006-08-29

    IPC分类号: C07H15/12

    CPC分类号: C07H15/04 C07H1/02

    摘要: Discloses is a process for producing α-D-glucopyranose, 3-O-decyl-2-deoxy-6-O-[2-deoxy-3-O-[(3R)-3-methoxydecyl]-6-O-methyl-2-[(11Z)-1-oxo-11-octadecenyl]amino]-4-O-phosphono-β-D-glucopyranosyl]-2-[(1,3-dioxotetradecyl)amino]- or 1-(dihydrogen phosphate) tetrasodium salt which is useful as an active ingredient of a pharmaceutical or an intermediate for the synthesis thereof, which is environment-friendly and excellent in safety, operationality and reproducibility. A process for producing a compound represented by the formula (I) comprising the steps of reacting a compound represented by the formula (VIII) with a palladium catalyst in the presence of a nucleopholic agent and treating the product with a sodium source.

    摘要翻译: 公开了一种生产±-D-吡喃葡萄糖,3-O-癸基-2-脱氧-6-O- [2-脱氧-3-O - [(3R)-3-甲氧基癸基] -6-O-甲基 -2 - [(11Z)-1-氧代-11-十八碳烯基]氨基] -4-O-膦酰基-2-D-吡喃葡萄糖基] -2 - [(1,3-二氧代十四烷基)氨基] - 或1-(二氢 磷酸盐)四钠盐,其可用作其合成的药物或中间体的活性成分,其环境友好并且安全性,可操作性和再现性优异。 一种制备由式(I)表示的化合物的方法,包括以下步骤:使式(VIII)表示的化合物与钯催化剂在一种核仁制剂存在下反应并用钠源处理该产物。