PROCESS FOR PRODUCTION OF LIPID A ANALOGUE
    1.
    发明申请
    PROCESS FOR PRODUCTION OF LIPID A ANALOGUE 审中-公开
    生产脂类似物的方法

    公开(公告)号:US20090149647A1

    公开(公告)日:2009-06-11

    申请号:US12064450

    申请日:2006-08-29

    CPC classification number: C07H15/04 C07H1/02

    Abstract: 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.

    Abstract translation: 公开了制备α-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-β-D-吡喃葡萄糖基] -2 - [(1,3-二氧代十四烷基)氨基] - 或1- 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,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类药剂的存在下反应并用钠源处理该产物。

    Process for the preparation of pyridine derivatives
    8.
    发明授权
    Process for the preparation of pyridine derivatives 失效
    吡啶衍生物的制备方法

    公开(公告)号:US06313303B1

    公开(公告)日:2001-11-06

    申请号:US09462180

    申请日:2000-01-03

    CPC classification number: C07D401/12

    Abstract: Processes for preparing sulfoxides useful as drugs such as acid secretion inhibitors or antiulcer drugs or intermediates for the preparation of drugs in high yields, at high purities, and with safety. Specifically, a process for the preparation of sulfoxides (II) by oxidizing a thio ether (I) with a peroxoborate salt in the presence of an acid anhydride or a metal catalyst; and a process for the preparation of sulfoxides (II) by oxidizing a thio ether (I) with an N-halosuccinimide, 1,3-dihalo-5,5-dimethyl-hydantoin or dichloroisocyanuric acid salt in the presence of a base. In said formulae R1 is hydrogen, methoxy or difluoromethoxy; R2 is methyl or methoxy; R3 is 3-methoxypropoxy, methoxy or 2,2,2-trifluoroethoxy; and R4 is hydrogen or methyl

    Abstract translation: 用于制备用作药物的亚砜的方法,例如酸分泌抑制剂或抗溃疡药物或用于以高产率,高纯度和安全性制备药物的中间体。 具体地说,在酸酐或金属催化剂存在下,用过氧硼酸盐氧化硫醚(I),制备亚砜(Ⅱ)的方法; 和通过在碱存在下用N-卤代琥珀酰亚胺,1,3-二卤代-5,5-二甲基 - 乙内酰脲或二氯异氰脲酸盐氧化硫醚(I)来制备亚砜(II)的方法。 在所述式中,R 1是氢,甲氧基或二氟甲氧基; R2是甲基或甲氧基; R3是3-甲氧基丙氧基,甲氧基或2,2,2-三氟乙氧基; R4为氢或甲基

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