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    PROCESS FOR THE PREPARATION OF (1S,4R)-2-OXA-3-AZABICYCLO[2,2.1]HEPT-5-ENES
    5.
    发明公开
    PROCESS FOR THE PREPARATION OF (1S,4R)-2-OXA-3-AZABICYCLO[2,2.1]HEPT-5-ENES 有权
    用于生产（1S，4R）-2-氧杂-3-氮杂双环[2.2.1]庚-5-恩恩

    公开(公告)号：EP2473492A1

    公开(公告)日：2012-07-11

    申请号：EP10747830.7

    申请日：2010-08-25

    申请人： Lonza Ltd

    发明人： FRANZEN, Manuela ,  NOTI, Christian

    IPC分类号： C07D265/34 ,  C07H5/00

    CPC分类号： C07D265/34 ,  Y02P20/55

    摘要： Enantiomerically enriched (1 S,4R)-2-oxa-3-azabicyclo[2.2.1]hept-5-ene of formula wherein PG
    1 is an amino-protective group, are prepared from cyclopentadiene via hetero-Diels-Alder cycloaddition with protected 1-
    C -nitroso-β-D-ribofuranosyl halides of formula wherein X is a halogen atom selected from fluorine, chlorine, bromine and iodine, PG
    2 is a hydroxyl-protective group and PG
    3 is a 1,2-diol-protective group.

    A COMBINATORIAL LIBRARY OF MOENOMYCIN ANALOGS AND METHODS OF PRODUCING SAME
    7.
    发明公开
    A COMBINATORIAL LIBRARY OF MOENOMYCIN ANALOGS AND METHODS OF PRODUCING SAME 审中-公开
    moenomycin类似物和方法的组合库中的

    公开(公告)号：EP1047703A1

    公开(公告)日：2000-11-02

    申请号：EP98960228.9

    申请日：1998-11-17

    申请人： Incara Pharmaceutical Corp.

    发明人： ALLANSON, Nigel, Mark ,  CHAN, Tin, Yau ,  HATZENBUHLER, Nicole, T. ,  JAIN, Rakesh, K. ,  KAKARLA, Ramesh ,  LIANG, Rui ,  LIU, Dashan ,  SILVA, Domingos ,  SOFIA, Michael

    IPC分类号： C07H1/00 ,  C07H5/00 ,  C07H15/00

    CPC分类号： C07H15/04 ,  C07H15/203 ,  C40B40/00

    摘要： A combinatorial chemical library of compounds structurally related to the moenomycin class of antibiotics has formula (I) wherein D is a donor mono- or disaccharide, A is an acceptor monosaccharide, and P-R is a lipophosphoglycerate mimetic group. Members of the library have a glycosidic linkage between the anomeric carbon of D and the C2 carbon of A, and the D-A moiety is in turn covalently linked through the anomeric carbon of A to the P-R group. Members of the library exhibit their greatest structural diversity in terms of substitutions occurring at the C3 position of the A residue, substitutions at the C2 position of the D residue, and different P-R groups used in assembling the compounds. Members of the library are preferably synthesized by solid phase techniques involving stepwise coupling of the respective units to a support, functionalizing the A and/or D saccharides either before or after immobilizing them on the support, and cleaving the assembled compounds from the support. Preferred functionalities attached to the sugar residues are amides, carbamates, ureas, sulfonamides, substituted amines, esters, carbonates, and sulfates. Exemplary P-R groups are derivatives of homoserine, glyceric acid, salicylates and mandelic acid. Members of the library can be screened for anti-microbial activity by contacting them with a culture of microbes and monitoring the growth rate of the microbes.

    Synthesis of intermediate useful in the preparation of nojirimycin and related compounds
    9.
    发明公开
    Synthesis of intermediate useful in the preparation of nojirimycin and related compounds 失效
    的中间体野尻霉素和相关化合物的制备的合成。

    公开(公告)号：EP0359263A2

    公开(公告)日：1990-03-21

    申请号：EP89117039.1

    申请日：1989-09-14

    申请人： MERRELL DOW PHARMACEUTICALS INC.

    发明人： Anzeveno, Peter B.

    IPC分类号： C07H9/04 ,  C07H5/00

    CPC分类号： C07H9/04

    摘要： 5-Amino-5-deoxy-1,2-O-isopropylidene-α-D-glucofuranose is conveniently prepared by a hydride reduction of 5-azido-­5-deoxy-1,2-O-isopropylidene-α-D-glucuronolactone and can readily be converted to nojirimycin, deoxynojirimycin or homonojirimycin.

    摘要翻译： 5-氨基-5-脱氧-1,2-O-异亚丙基的α--D-呋喃葡萄糖可方便地由一氢化物还原5-叠氮基-5-脱氧-1,2-O-异亚丙基的α-D-葡糖醛酸内酯的制备 和可被转化为随手野尻霉素，脱氧野尻霉素或homonojirimycin。

    Isolation of unreduced oligosaccharides
    10.
    发明公开
    Isolation of unreduced oligosaccharides 失效
    未还原的低聚糖的分离。

    公开(公告)号：EP0215766A2

    公开(公告)日：1987-03-25

    申请号：EP86870123.6

    申请日：1986-09-05

    申请人： Monsanto Company

    发明人： Dwek, Raymond Allen ,  Rademacher, Thomas William

    IPC分类号： C13K13/00 ,  C07H5/00 ,  C07H3/06

    CPC分类号： C07K9/005 ,  C13K13/00

    摘要： A preparative scale method for the isolation of unreduced oligosaccharides of glycoproteins and glycohormones having a N-linked oligosaccharide structure is disclosed. The method employs hydrazin­olysis of the glycoprotein or glycohormone under reaction conditions to cause cleavage at the N-linked sites, producing a mixture having as a major component a de-N-acetylated hydrazone derivative of the oligo­saccharides, followed by N-acylation of the hydrazone derivative, acid-catalysis of the hydrazone derivative to produce unreduced oligosaccharides, and subjecting the resulting unreduced oligosaccharides to cellulose column chromatography to remove contaminants and to recover the unreduced oligosaccharides.