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1. 发明授权

US08669382B2 Method for producing (2R)-2-fluoro-2-C-methyl-D-ribono-γ-lactone precursor 有权
标题翻译：（2R）-2-氟-2-C-甲基-D-内罗糖-γ-内酯前体的制备方法
公开(公告)号：US08669382B2
公开(公告)日：2014-03-11
申请号：US13697691
申请日：2011-04-25
申请人： Akihiro Ishii , Hirokatsu Nagura , Hideyuki Tsuruta
发明人： Akihiro Ishii , Hirokatsu Nagura , Hideyuki Tsuruta
IPC分类号： C07D317/10
CPC分类号： C07D317/30 , Y02P20/55
摘要： In the presence invention, a (2R)-2-fluoro-2-C-methyl-D-ribono-γ-lactone precursor is produced in the form of a ring-opened fluorinated compound by reaction of a 1,2-diol with sulfuryl fluoride (SO2F2) in the presence of an organic base and, optionally, a fluoride ion source. The production method of the present invention secures less number of process steps as compared to the conventional production method (shortening of three steps: cyclic sulfurous esterification, oxidation and ring-opening fluorination to one step) and satisfies the requirements for industrial production (high yield and high reproductivity). The thus-obtained (2R)-2-fluoro-2-C-methyl-D-ribono-γ-lactone precursor is useful as an important intermediate for the synthesis of 2′-deoxy-2′-fluoro-2′-C-methylcytidine with antivirus activity.
摘要翻译：在本发明的存在下，通过1,2-二醇与式（Ⅱ）的反应制备开环氟化合物形式的（2R）-2-氟-2-C-甲基-D-内罗糖-γ-内酯前体硫酰氟（SO 2 F 2）在有机碱和任选的氟离子源存在下进行。本发明的制造方法与现有的制造方法（缩短三个步骤：环状亚硫酸酯化，氧化和开环氟化至一步）相比确保了较少的工艺步骤，并且满足了工业生产的要求（高产率和高繁殖力）。由此获得的（2R）-2-氟-2-C-甲基-D-内罗糖-γ-内酯前体可用作合成2'-脱氧-2'-氟-2'-碳甲基胞苷具有抗病毒活性。

2. 发明申请

US20130072699A1 Method for Producing (2R)-2-Fluoro-2-C-Methyl-D-Ribono-y-Lactone Precursor 有权
标题翻译：（2R）-2-氟-2-C-甲基-D-内酰基-γ-内酯前体的制备方法
公开(公告)号：US20130072699A1
公开(公告)日：2013-03-21
申请号：US13697691
申请日：2011-04-25
申请人： Akihiro Ishii , Hirokatsu Nagura , Hideyuki Tsuruta
发明人： Akihiro Ishii , Hirokatsu Nagura , Hideyuki Tsuruta
IPC分类号： C07D317/30
CPC分类号： C07D317/30 , Y02P20/55
摘要： In the presence invention, a (2R)-2-fluoro-2-C-methyl-D-ribono-γ-lactone precursor is produced in the form of a ring-opened fluorinated compound by reaction of a 1,2-diol with sulfuryl fluoride (SO2F2) in the presence of an organic base and, optionally, a fluoride ion source. The production method of the present invention secures less number of process steps as compared to the conventional production method (shortening of three steps: cyclic sulfurous esterification, oxidation and ring-opening fluorination to one step) and satisfies the requirements for industrial production (high yield and high reproductivity). The thus-obtained (2R)-2-fluoro-2-C-methyl-D-ribono-γ-lactone precursor is useful as an important intermediate for the synthesis of 2′-deoxy-2′-fluoro-2′-C-methylcytidine with antivirus activity.
摘要翻译：在本发明的存在下，通过1,2-二醇与（II）的反应制备开环氟化合物的形式的（2R）-2-氟-2-C-甲基-D-内罗糖-γ-内酯前体硫酰氟（SO 2 F 2）在有机碱和任选的氟离子源存在下进行。本发明的制造方法与现有的制造方法（缩短三个步骤：环状亚硫酸酯化，氧化和开环氟化至一步）相比确保了较少的工艺步骤，并且满足了工业生产的要求（高产率和高繁殖力）。由此获得的（2R）-2-氟-2-C-甲基-D-内克隆-γ-内酯前体可用作合成2'-脱氧-2'-氟-2'-C 甲基胞苷具有抗病毒活性。

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