VERFAHREN ZUR HERSTELLUNG VON 2'-O-FUCOSYLLACTOSE

    公开(公告)号:EP3411379A1

    公开(公告)日:2018-12-12

    申请号:EP17703388.3

    申请日:2017-02-02

    申请人: BASF SE

    摘要: The present invention relates to a process for producing 2'-O-fucosyllactose, to the intermediates obtainable by this process and to the use of these intermediates. Production comprises the reaction of a protected fucose of general formula (I) with a tri-(C
    1 -C
    6 -alkyl)silyl iodide to form a protected 1-iodofucose followed by reaction of the protected 1-iodofucose with a compound of general formula (I I), in the presence of at least one base and deprotection of the obtained coupling product to obtain 2'-O-fucosyllactose. The variables are defined as follows: R
    a and R
    b are identical or different and represent -C(=O)-C
    1 -C
    6 -alkyl or -C(=O)-phenyl, wherein phenyl is unsubstituted or optionally comprises 1 to 5 substituents or R
    a and R
    b together represent a -(C=O)- radical or a substituted methylene radical -C(R
    d R
    e )-, R
    c represents an R
    Si radical or benzyl, wherein benzyl is unsubstituted or optionally bears 1, 2 or 3 substituents, R
    Si represents a radical of formula SiR
    f R
    g R
    h , wherein R
    f , R
    g and R
    h are identical or different and represent, for example C
    1 -C
    8 -alkyl, R
    1 represents a -C(=O)-R
    11 radical or a SiR
    12 R
    13 R
    14 radical, R
    2 are identical or different and represent for example C
    1 -C
    8 -alkyl, R
    3 are identical or different and represent for example C
    1 -C
    8 -alkyl or both radicals R
    3 together represent linear C
    1 -C
    4 -alkenyl which is unsubstituted or bears 1 to 6 methyl groups as substituents.

    METHOD OF PURIFYING IDRAPARINUX SODIUM
    18.
    发明公开
    METHOD OF PURIFYING IDRAPARINUX SODIUM 审中-公开
    净化IDRAPARINUX SODIUM的方法

    公开(公告)号:EP3201210A2

    公开(公告)日:2017-08-09

    申请号:EP15846879.3

    申请日:2015-09-30

    IPC分类号: C07H15/04 C07H15/18 C07H15/14

    CPC分类号: C07H1/06 C07H15/04

    摘要: A method for the purification of idraparinux sodium includes: passing a solution including a crude idraparinux sodium through a column including a sodium ion exchange resin to obtain a first mixture; passing a solution including the first mixture through a gel chromatogaphy column to obtain a second mixture; and precipitating a purified idraparinux sodium from a solution including the second mixture.

    摘要翻译: 用于精制伊达拉滨克斯钠的方法包括:使包含粗伊达令林钠的溶液通过包含钠离子交换树脂的柱以获得第一混合物; 将包含第一混合物的溶液通过凝胶色谱柱以获得第二混合物; 并从包含第二混合物的溶液中沉淀纯化的伊达肝素钠。

    METHOD FOR PRODUCTING THIOLANE SKELETON-TYPE GLYCOCONJUGATE, AND THIOLANE SKELETON-TYPE GLYCOCONJUGATE
    19.
    发明公开
    METHOD FOR PRODUCTING THIOLANE SKELETON-TYPE GLYCOCONJUGATE, AND THIOLANE SKELETON-TYPE GLYCOCONJUGATE 有权
    VERFAHREN ZUR HERSTELLUNG EINES THIOLANSKELETTARTIGEN GLYCOKONJUGATS UND THIOLANSKELETTARTIGES GLYCOKONJUGAT

    公开(公告)号:EP3109245A4

    公开(公告)日:2017-03-01

    申请号:EP15751503

    申请日:2015-02-17

    申请人: FUJIFILM CORP

    摘要: There is provided a production method of a compound represented by the following formula (II) through a step of reacting a compound represented by the following General Formula (I) with a sulfur compound. In General Formulas (I) and (II), R 1 represents a hydrogen atom or an acyl group, R 2 represents a hydrogen atom, a fluorine atom, an acyloxy group, an arylmethyloxy group, an allyloxy group, an arylmethyloxycarbonyloxy group, or an allyloxycarbonyloxy group, R 3 represents a hydrogen atom or an acyloxy group, R 5 represents an alkyl group or an aryl group, and X represents a leaving group. Here, in a case where R 2 is a fluorine atom, an acyloxy group, an arylmethyloxy group, an allyloxy group, an arylmethyloxycarbonyloxy group, or an allyloxycarbonyloxy group, R 3 is an acyloxy group.

    摘要翻译: 通过使由下列通式(I)表示的化合物与硫化合物反应的步骤,提供由下式(II)表示的化合物的制备方法。 在通式(I)和(II)中,R 1表示氢原子或酰基,R 2表示氢原子,氟原子,酰氧基,芳基甲氧基,烯丙氧基,芳基甲氧基羰基氧基或 烯丙氧基羰基氧基,R 3表示氢原子或酰氧基,R 5表示烷基或芳基,X表示离去基团。 这里,在R 2为氟原子,酰氧基,芳基甲氧基,烯丙氧基,芳基甲氧基羰基氧基或烯丙氧基羰基氧基的情况下,R 3为酰氧基。