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10 条记录 (耗时 0.011 秒)

    Improvements in or relating to 2',2'-difluoronucleosides
    1.
    发明公开
    Improvements in or relating to 2',2'-difluoronucleosides 失效
    2' ，2'-二氟核苷。

    公开(公告)号：EP0306190A2

    公开(公告)日：1989-03-08

    申请号：EP88307750.5

    申请日：1988-08-22

    申请人： ELI LILLY AND COMPANY

    发明人： Chou, Ta-Sen ,  Heath, Perry Clark ,  Patterson, Lawrence Edward

    IPC分类号： C07H7/027 ,  C07H13/08 ,  C07H19/073 ,  C07H19/04

    CPC分类号： C07D307/33 ,  C07H19/06 ,  Y02P20/55

    摘要： The present invention provides a process for preparing lactone intermediates to 2′,2′-difluoronucleo­sides whereby reversion back to the lactone's open chain precursor is minimized and the desired erythro enantiomer can be selectively isolated from an enantiomeric mixture of erythro and threo lactones in crystalline form. Also provided is a process for producing 2′-deoxy-2′,2′-­difluoronucleosides in about a 1:1 α/β anomeric ratio, and processes for selectively isolating β-2′-deoxy-2′,2′-­difluorocytidine, or an organic or inorganic acid addi­tion salt thereof, from the 1:1 α/β mixture.

    摘要翻译： 本发明提供了制备内酯中间体至2分钟，2分钟 - 二氟核苷的方法，由此反转回内酯的开链前体被最小化，并且可以从结晶形式的赤式和苏式内酯的对映异构体混合物中选择性分离所需的赤式对映异构体 。 还提供了以约1：1的α/β端基异构体比例生产2分钟脱氧-2分钟，2分钟的二氟核苷的方法，以及选择性分离β-2分钟脱氧-2分钟，2分钟 - 二氟胞苷 ，或其有机或无机酸加成盐，来自1:1的α/β混合物。

    Improvements in or relating to 2',2'-difluoronucleosides
    4.
    发明公开
    Improvements in or relating to 2',2'-difluoronucleosides 失效
    改善或相关于2'，2'-二氟尿嘧啶

    公开(公告)号：EP0306190A3

    公开(公告)日：1991-11-21

    申请号：EP88307750.5

    申请日：1988-08-22

    申请人： ELI LILLY AND COMPANY

    发明人： Chou, Ta-Sen ,  Heath, Perry Clark ,  Patterson, Lawrence Edward

    IPC分类号： C07H7/027 ,  C07H13/08 ,  C07H19/073 ,  C07H19/04

    CPC分类号： C07D307/33 ,  C07H19/06 ,  Y02P20/55

    摘要： The present invention provides a process for preparing lactone intermediates to 2′,2′-difluoronucleo­sides whereby reversion back to the lactone's open chain precursor is minimized and the desired erythro enantiomer can be selectively isolated from an enantiomeric mixture of erythro and threo lactones in crystalline form. Also provided is a process for producing 2′-deoxy-2′,2′-­difluoronucleosides in about a 1:1 α/β anomeric ratio, and processes for selectively isolating β-2′-deoxy-2′,2′-­difluorocytidine, or an organic or inorganic acid addi­tion salt thereof, from the 1:1 α/β mixture.

    Synthesis of benzo(f)quinolinones
    5.
    发明公开
    Synthesis of benzo(f)quinolinones 失效
    苯并（F）chinolinone-SYNTHESE

    公开(公告)号：EP0839807A1

    公开(公告)日：1998-05-06

    申请号：EP97308644.0

    申请日：1997-10-29

    申请人： ELI LILLY AND COMPANY

    发明人： Brennan, John ,  Doecke, Christopher William ,  Heath, Perry Clark ,  Patterson, Lawrence Edward ,  Udodong, Uko Effiong ,  Weigel, Leland Otto

    IPC分类号： C07D221/10 ,  C07C323/22

    CPC分类号： C07D417/12 ,  C07C319/14 ,  C07C319/20 ,  C07C323/22 ,  C07C2602/10 ,  C07D221/10 ,  C07C323/21 ,  C07C323/38 ,  C07C323/62

    摘要： A process for preparing intermediates and benzoquinolin-3-one pharmaceuticals, of the following formula I:
    wherein R 1 represents:
    2-nitrophenyl, 4-nitrophenyl, 2-cyanophenyl, 4-cyanophenyl, 2-nitronaphthyl, 4-nitronaphthyl, 2-cyanonaphthyl, 4-cyanonaphthyl, 2-quinolinyl, 4-quinolinyl, 7-quinolinyl, 1-isoquinolinyl, 3-isoquinolinyl, 8-isoquinolinyl, 2-quinoxalinyl, 2-benzothiazolyl, 3-1H-indazolyl, 2-benzoxazolyl, 3-1,2-benzisothiazolyl, 2-pyridinyl, 4-pyridinyl, 2-pyrazinyl, 2-naphtho[2,3-d]thiazolyl, 2-naphto[1,2-d]thiazolyl, 9-anthryl, 2-thiazolyl, 2-benzimidazolyl, 1-benz[g]isoquinolinyl, 8-benz[g]isoquinolinyl, 5-1H-tetrazolyl, 2-quinazolinyl, 2-thiazolo[4,5-b]pyridinyl, 4-10H-pyridazino[3,2-b]-2-quinazolinyl, 2-1,4-benzodioxinyl, 2-triazine, 2-benzoxazine, 4-benzoxazine, 2-purine or 8-purine.
    Such pharmaceuticals are effective in treating conditions consequent on 5α-reductase.

    摘要翻译： 制备下式I的中间体和苯并喹啉-3-酮药物的方法：其中R 1表示：2-硝基苯基，4-硝基苯基，2-氰基苯基，4-氰基苯基，2-硝基萘基，4 2-硝基萘基，2-氰基萘基，4-氰基萘基，2-喹啉基，4-喹啉基，7-喹啉基，1-异喹啉基，3-异喹啉基，8-异喹啉基，2-喹喔啉基，2-苯并噻唑基，3-1H-吲唑基， - 苯并恶唑基，3-1,2-苯并异噻唑基，2-吡啶基，4-吡啶基，2-吡嗪基，2-萘并[2,3]恶噻唑基，2-萘并[1,2]噻唑基，9-蒽基，2-噻唑基，2-苯并咪唑基 ，1-苯并异喹啉基，8-苯并异喹啉基，5-1H-四唑基，2-喹唑啉基，2-噻唑并[4,5-b]吡啶基，4-10H-哒嗪基-3,3,2-b] -2-喹唑啉基，2-1,4-苯并二恶英基，2 3-三嗪，2-苯并恶嗪，4-苯并恶嗪，2-嘌呤或8-嘌呤。 这样的药物在治疗5α-还原酶的病症方面是有效的。

    Method for preparing 2',deoxy-2',2'-difluornucleosides
    6.
    发明公开
    Method for preparing 2',deoxy-2',2'-difluornucleosides 失效
    为2'-脱氧-2的制备2'-二氟核苷过程”，

    公开(公告)号：EP0688783A1

    公开(公告)日：1995-12-27

    申请号：EP95201846.3

    申请日：1988-08-22

    申请人： ELI LILLY AND COMPANY

    发明人： Chou, Ta Sen ,  Heath, Perry Clark ,  Patterson, Lawrence Edward

    IPC分类号： C07H19/04 ,  C07H13/08

    CPC分类号： C07D307/33 ,  C07H19/06 ,  Y02P20/55

    摘要： The present invention provides a process for preparing lactone intermediates to 2',2'-difluoronucleosides whereby reversion back to the lactone's open chain precursor is minimized and the desired erythro enantiomer can be selectively isolated from an enantiomeric mixture of erythro and threo lactones in crystalline form. Also provided is a process for producing 2'-deoxy-2',2'-difluoronucleosides in about a 1:1 α/β anomeric ratio, and processes for selectively isolating β-2'-deoxy-2',2'-difluorocytidine, or an organic or inorganic acid addition salt thereof, from the 1:1 α/β mixture.

    Stereoselective process for preparing protected 2',2'-difluorolactonen
    9.
    发明公开
    Stereoselective process for preparing protected 2',2'-difluorolactonen 失效
    对于受保护的2”，2'- difluorlactonen的制备方法立体选择性

    公开(公告)号：EP0688782A1

    公开(公告)日：1995-12-27

    申请号：EP95201845.5

    申请日：1988-08-22

    申请人： ELI LILLY AND COMPANY

    发明人： Chou, Ta-Sen ,  Heath, Perry Clark ,  Patterson, Lawrence Edward

    IPC分类号： C07H19/04 ,  C07H13/08

    CPC分类号： C07D307/33 ,  C07H19/06 ,  Y02P20/55

    摘要： The present invention provides a process for preparing lactone intermediates to 2',2'-difluoronucleosides whereby reversion back to the lactone's open chain precursor is minimized and the desired erythro enantiomer can be selectively isolated from an enantiomeric mixture of erythro and threo lactones in crystalline form. Also provided is a process for producing 2'-deoxy-2',2'-difluoronucleosides in about a 1:1 α/β anomeric ratio, and processes for selectively isolating β-2'-deoxy-2',2'-difluorocytidine, or an organic or inorganic acid addition salt thereof, from the 1:1 α/β mixture.

    Process for selectively isolating bêta-2'-deoxy-2',2'-difluorocytidine or its salts
    10.
    发明公开
    Process for selectively isolating bêta-2'-deoxy-2',2'-difluorocytidine or its salts 失效
    Verfahren zur selektiven Isolierung von B-2'-desoxy-2'2'-二氟胞苷和其他服务员Salze。

    公开(公告)号：EP0630905A1

    公开(公告)日：1994-12-28

    申请号：EP94202041.3

    申请日：1988-08-22

    申请人： ELI LILLY AND COMPANY

    发明人： Chou, Ta-Sen ,  Heath, Perry Clark ,  Patterson, Lawrence Edward

    IPC分类号： C07H19/04

    CPC分类号： C07D307/33 ,  C07H19/06 ,  Y02P20/55

    摘要： The present invention provides a process for preparing lactone intermediates to 2',2'-difluoronucleosides whereby reversion back to the lactone's open chain precursor is minimized and the desired erythro enantiomer can be selectively isolated from an enantiomeric mixture of erythro and threo lactones in crystalline form. Also provided is a process for producing 2'-deoxy-2',2'-difluoronucleosides in about a 1:1 α/β anomeric ratio, and processes for selectively isolating β-2'-deoxy-2',2'-difluorocytidine, or an organic or inorganic acid addition salt thereof, from the 1:1 α/β mixture.

    摘要翻译： 本发明提供了制备2'，2'-二氟核苷的内酯中间体的方法，由此反转回内酯的开链前体被最小化，并且可以从结晶形式的赤式和苏式内酯的对映异构体混合物中选择性分离所需的赤式对映异构体 。 还提供了以约1：1的α/β端基异构体比率生产2'-脱氧-2'，2'-二氟核苷的方法，以及选择性分离β-2'-脱氧-2'，2'-二氟胞苷 ，或其有机或无机酸加成盐，来自1:1的α/β混合物。