-
公开(公告)号:US5434254A
公开(公告)日:1995-07-18
申请号:US49220
申请日:1993-04-19
IPC分类号: C07D307/33 , C07H19/06 , C07H19/00
CPC分类号: C07D307/33 , C07H19/06
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 .alpha./.beta. anomeric ratio, and processes for selectively isolating .beta.-2'-deoxy-2',2'-difluorocytidine, or an organic or inorganic acid addition salt thereof, from the 1:1 .alpha./.beta. 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,由此使内酯的开链前体的回复被最小化,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出所需的赤式对映异构体 。 还提供了以大约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。
-
公开(公告)号:US4965374A
公开(公告)日:1990-10-23
申请号:US445139
申请日:1989-12-04
IPC分类号: C07D307/33 , C07H19/06
CPC分类号: C07D307/33 , C07H19/06
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 .alpha./.beta. anomeric ratio, and processes for selectively isolating .beta.-2'-deoxy-2',2'-difluorocytidine, or an organic or inorganic acid addition salt thereof, from the 1:1 .alpha./.beta. 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,由此使内酯的开链前体的回复被最小化,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出所需的赤式对映异构体 。 还提供了以大约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。
-