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专利信息

专利号:US-8669382-B2
优先权日:2010-06-03
标题 :Method for producing (2R)-2-fluoro-2-C-methyl-D-ribono-γ-lactone precursor
发明人：ISHII AKIHIRO; NAGURA HIROKATSU; TSURUTA HIDEYUKI
权利人:ISHII AKIHIRO; NAGURA HIROKATSU; TSURUTA HIDEYUKI; CENTRAL GLASS CO LTD
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 (SO 2 F 2 ) 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.