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.
专利号:US-2009281161-A1 优先权日:2006-06-13 标 题:Organic Compounds 发明人:MAIBAUM JUERGEN KLAUS; LORTHIOIS EDWIGE LILIANE JEANNE 权利人:MAIBAUM JUERGEN KLAUS; LORTHIOIS EDWIGE LILIANE JEANNE 摘要:Novel 3,4-di-, 3,3,4-di-, 3,4,4,-tri- and 3,3,4,4-tetra-substituted pyrrolidine compounds, these compounds for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease (=disorder) that depends on inappropriate activity of renin; the use of a compound of that class for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on inappropriate activity of renin; the use of a compound of that class in the treatment of a disease that depends on inappropriate activity of renin; pharmaceutical formulations comprising a said substituted pyrrolidine compound, and/or a method of treatment comprising administering a said substituted pyrrolidine compound, a method for the manufacture of said substituted pyrrolidine compounds, and novel intermediates and partial steps for their synthesis are described. The substituted pyrrolidine compounds are especially of the formula (I) wherein the substituents are as described in the specification.
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