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    PROCESS FOR THE PREPARATION OF (1S,4R)-2-OXA-3-AZABICYCLO[2,2.1]HEPT-5-ENES
    2.
    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.