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1. 发明申请

US20100069625A1 PROCESS FOR PREPARING OF 2'-DEOXY-2'2'-DIFLUOROCYTIDINE 失效
标题翻译：制备2'-脱氧-2'-脱氧胆碱的方法
公开(公告)号：US20100069625A1
公开(公告)日：2010-03-18
申请号：US12532331
申请日：2008-03-20
申请人： Su-Jin Park , Chun-Rim Oh , Young-Deuck Kim
发明人： Su-Jin Park , Chun-Rim Oh , Young-Deuck Kim
IPC分类号： C07H19/06 , C07H3/02 , C07D317/08
CPC分类号： C07H1/00 , C07H19/06 , Y02P20/55
摘要： Disclosed is a method for preparing 2′-deoxy-2′,2′-difluorocytidine of Formula I comprising, preparing an optically pure 3R-hydroxypropane amide compound of Formula VIII from an optical ester compound of Formula IX using an optically active chiral amine, preparing an optically pure D-erythro-2,2-difluoro-2-deoxy-1-oxoribose compound of Formula V from the compound of Formula VIII, glycosylating the compound of Formula V with a nucleobase to prepare the 2′-deoxy-2′,2′-difluorocytidine of Formula I as a β-nucleoside. With the present invention, it is possible to prepare an optically pure compound of Formula I in a high purity and a high yield. In the Formulae, R1 and R2 are protecting groups and are each independently benzoyl, 4-methylbenzoyl, 3-methylbenzoyl, 4-cyanobenzoyl, 3-cyanobenzoyl, 4-propylbenzoyl, 2-ethoxybenzoyl, 4-t-butylbenzoyl, 1-naphthoyl or 2-naphthoyl, R3, R4 and R7 are each independently C1-C3 alkyl, R5 is methyl or ethyl, R6 is hydrogen, methyl or methoxy.
摘要翻译：公开了一种制备式I的2'-脱氧-2'，2'-二氟胞苷的方法，其包括：使用光学活性手性胺由式IX的光学酯化合物制备光学纯的3R-羟基丙酰胺化合物，从式VIII化合物制备光学纯的D-型赤式-2,2-二氟-2-脱氧-1-氧代核糖核糖化合物，用式I化合物将式V化合物糖基化，从而制备2'-脱氧-2 '，式Ⅰ的2'-二氟胞苷作为核苷。通过本发明，可以以高纯度和高收率制备光学纯的式I化合物。在式中，R 1和R 2是保护基，各自独立地是苯甲酰基，4-甲基苯甲酰基，3-甲基苯甲酰基，4-氰基苯甲酰基，3-氰基苯甲酰基，4-丙基苯甲酰基，2-乙氧基苯甲酰基，4-叔丁基苯甲酰基，1-萘甲酰基或 2-萘甲酰基，R3，R4和R7各自独立地为C1-C3烷基，R5为甲基或乙基，R6为氢，甲基或甲氧基。

2. 发明授权

US07994310B2 Process for preparing 2′-deoxy-2′, 2′-difluorocytidine 失效
标题翻译：制备2'-脱氧-2'，2'-二氟胞苷的方法
公开(公告)号：US07994310B2
公开(公告)日：2011-08-09
申请号：US12532331
申请日：2008-03-20
申请人： Su-Jin Park , Chun-Rim Oh , Young-Deuck Kim
发明人： Su-Jin Park , Chun-Rim Oh , Young-Deuck Kim
IPC分类号： C07H19/073
CPC分类号： C07H1/00 , C07H19/06 , Y02P20/55
摘要： Disclosed is a method for preparing 2′-deoxy-2′,2′-difluorocytidine of Formula I comprising, preparing an optically pure 3R-hydroxypropane amide compound of Formula VIII from an optical ester compound of Formula IX using an optically active chiral amine, preparing an optically pure D-erythro-2,2-difluoro-2-deoxy-1-oxoribose compound of Formula V from the compound of Formula VIII, glycosylating the compound of Formula V with a nucleobase to prepare the 2′-deoxy-2′,2′-difluorocytidine of Formula I as a β-nucleoside. With the present invention, it is possible to prepare an optically pure compound of Formula I in a high purity and a high yield. In the Formulae, R1 and R2 are protecting groups and are each independently benzoyl, 4-methylbenzoyl, 3-methylbenzoyl, 4-cyanobenzoyl, 3-cyanobenzoyl, 4-propylbenzoyl, 2-ethoxybenzoyl, 4-t-butylbenzoyl, 1-naphthoyl or 2-naphthoyl, R3, R4 and R7 are each independently C1-C3 alkyl, R5 is methyl or ethyl, R6 is hydrogen, methyl or methoxy.
摘要翻译：公开了一种制备式I的2'-脱氧-2'，2'-二氟胞苷的方法，其包括：使用光学活性手性胺由式IX的光学酯化合物制备光学纯的3R-羟基丙酰胺化合物，从式VIII化合物制备光学纯的D-型赤式-2,2-二氟-2-脱氧-1-氧代核糖核糖化合物，用式I化合物将式V化合物糖基化，从而制备2'-脱氧-2 '，式I的2'-二氟胞苷作为核苷。通过本发明，可以以高纯度和高收率制备光学纯的式I化合物。在式中，R 1和R 2是保护基，各自独立地是苯甲酰基，4-甲基苯甲酰基，3-甲基苯甲酰基，4-氰基苯甲酰基，3-氰基苯甲酰基，4-丙基苯甲酰基，2-乙氧基苯甲酰基，4-叔丁基苯甲酰基，1-萘甲酰基或 2-萘甲酰基，R3，R4和R7各自独立地为C1-C3烷基，R5为甲基或乙基，R6为氢，甲基或甲氧基。

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