1-ALPHA-HALO-2,2-DIFLUORO-2-DEOXY-D-RIBOFURANOSE DERIVATIVES AND PROCESS FOR THE PREPARATION THEREOF
    5.
    发明公开
    1-ALPHA-HALO-2,2-DIFLUORO-2-DEOXY-D-RIBOFURANOSE DERIVATIVES AND PROCESS FOR THE PREPARATION THEREOF 审中-公开
    1-ALPHA-2,2,2-二氟-2-脱氧-D-呋喃葡萄糖糖衍生物及其制备方法

    公开(公告)号:EP1781678A1

    公开(公告)日:2007-05-09

    申请号:EP05756757.0

    申请日:2005-06-21

    IPC分类号: C07H3/08

    CPC分类号: C07H3/08

    摘要: 1-α-halo-2,2-difluoro-2-deoxy-D-ribofuranose derivative of formula (I) having the 3-hydroxy group protected with a biphenylcarbonyl group is a solid which can be easily purified by a simple procedure such as recrystallization, and therefore, it can be advantageously used as an intermediate in the preparation of gemcitabine in a large scale. Further, the 1-α-halo-2,2-difluoro-2-deoxy-D-ribofuranose derivative of formula (I) can be prepared with high stereoselectivity using the compound of formula (V) as an intermediate.

    摘要翻译: 具有用联苯基羰基保护的3-羟基的式(I)的1-α-卤代-2,2-二氟-2-脱氧-D-呋喃核糖衍生物是一种固体,其可以通过简单的方法容易地纯化 作为重结晶,因此它可以有利地用作大规模制备吉西他滨的中间体。 此外,可以使用式(V)化合物作为中间体,以高立体选择性制备式(I)的1-α-卤代-2,2-二氟-2-脱氧-D-呋喃核糖衍生物。

    Immuno-suppressing enepyranose derivatives
    7.
    发明公开
    Immuno-suppressing enepyranose derivatives 失效
    免疫抑制剂。

    公开(公告)号:EP0560055A1

    公开(公告)日:1993-09-15

    申请号:EP93101822.0

    申请日:1993-02-05

    摘要: An immuno-suppressive agent containing, as an effective component, an enopyranose derivative of the following formula (I) or its salt:
    wherein R 1 is a hydrogen atom, alkyl which may be substituted, alkenyl, alkynyl, -OSO 2 R 7 , a halogen atom, -OCOR 7 , -NHCOR 8 , alkoxy, phenyl which may be substituted or a saccharose residue, R 2 is a hydrogen atom or alkyl, R 3 is a hydrogen atom or a halogen atom, R 4 is a hydrogen atom, -COR 9 , silyl which may be substituted or alkyl which may be substituted, one of R 5 and R 6 is hydroxyl, alkoxy which may be substituted, a saccharose residue, cycloalkyloxy which may be substituted or -OCOR 10 and the other is a hydrogen atom or alkyl which may be substituted, or R 4 and R 5 together form a single bond, while R 6 is a hydrogen atom or alkyl which may be substituted, each of R 7 , R 9 and R 10 is alkyl or phenyl which may be substituted, R 8 is alkyl, phenyl which may be substituted or benzyloxy, X is a hydrogen atom, alkyl which may be substituted, alkenyl which may be substituted, alkynyl which may be substituted, cycloalkyl which may be substituted, phenyl which may be substituted, pyridyl which may be substituted, furanyl which may be substituted, thienyl which may be substituted, formyl, -COR 11 , -C(W 1 )W 2 R 11 or -SO 2 R 11 , R 11 is a chain hydrocarbon group which may be substituted, a monocyclic hydrocarbon group which may be substituted, a polycyclic hydrocarbon group which may be substituted, a monocyclic heterocycle group which may be substituted, or a polycyclic heterocycle group which may be substituted, W 1 is an oxygen atom or a sulfur atom, W 2 is an oxygen atom, a sulfur atom or -NH-, Y is a hydrogen atom, alkyl which may be substituted, alkenyl which may be substituted or alkynyl which may be substituted.

    摘要翻译: 含有作为有效成分的下式(I)的吡喃葡萄糖衍生物或其盐的免疫抑制剂:其中R 1为氢原子,可被取代的烷基,烯基,炔基, - OSO 2 R 7,卤素原子,-OCOR 7,-NHCOR 8,烷氧基,可被取代的苯基或蔗糖残基,R 2是氢原子或烷基,R 3是 氢原子或卤素原子,R 4是氢原子,-COR 9,可被取代的甲硅烷基或可被取代的烷基,R 5和R 6之一是羟基,烷氧基 可以被取代,可以被取代的蔗糖残基,可以被取代的环烷氧基或-OCOR 1,另一个是可以被取代的氢原子或烷基,或者R 4和R 5一起形成一个 键,而R 6为氢原子或可被取代的烷基,R 7,R 9和R 10各自为可被取代的烷基或苯基,R 8, 是烷基,可被取代的苯基或苄氧基,X是氢原子,烷基 可被取代的烯基,可被取代的链烯基,可被取代的环烷基,可被取代的苯基,可被取代的吡啶基,可被取代的呋喃基,可被取代的噻吩基,甲酰基, -COR 1,-C(W 1)W 2 R 1或-SO 2 R 1,R 1是链烃基 可被取代的单环烃基,可被取代的多环烃基,可被取代的多环烃基,可被取代的单环杂环基或可被取代的多环杂环基,W 1是氧原子 或硫原子,W 2为氧原子,硫原子或-NH-,Y为氢原子,可被取代的烷基,可被取代的烯基或可被取代的炔基。

    CARBOHYDRATE PROCESS.
    8.
    发明公开
    CARBOHYDRATE PROCESS. 失效
    VERFAHREN MITTELS KARBOHYDRATEN。

    公开(公告)号:EP0056038A4

    公开(公告)日:1982-12-09

    申请号:EP81901961

    申请日:1981-06-18

    摘要: Methods of producing glucosone which comprises enzymatically oxidizing glucose with glucose-2-oxidase in a first zone and separating the concomitantly produced hydrogen peroxide from said first zone through a semi-permeable membrane into a second zone, said membrane being permeable only to compounds of a molecular weight of less than about 100.

    摘要翻译: 生产葡萄糖醛的方法包括在第一区中用葡萄糖-2-氧化酶酶促葡萄糖氧化,并将伴随产生的过氧化氢从所述第一区经过半透膜分离到第二区中,所述膜仅可渗透至 分子量小于约100。