专利号:US-2023286918-A1 优先权日:2020-07-02 标 题:Manufacturing process for 3,5-dichloropicolinonitrile for synthesis of vadadustat 发明人:JURKAUSKAS VALDAS; JUNG YOUNG CHUN; KWON TAESOO; KANNAN ARUNACHALAM; GONDI VIJAYA BHASKER 权利人:AKEBIA THERAPEUTICS INC 摘要:Disclosed herein are methods and processes of preparing vadadustat or a pharmaceutically acceptable salts thereof, and intermediates (e.g., a compound of Formula (I), (I-F), (II), or (IV), or a pharmaceutically acceptable salts thereof) useful for the synthesis of vadadustat.
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-2013310403-A1 优先权日:2012-05-15 标题 :Fluoro-homoneplanocin A and nucleoside derivatives, method for the synthesis thereof, and the pharmaceutical compositions comprising the same as an active component for treatment of cancer
专利号:US-9120760-B2 优先权日:2012-05-15 标 题 :Fluoro-homoneplanocin A and nucleoside derivatives, method for the synthesis thereof, and the pharmaceutical compositions comprising the same as an active component for treatment of cancer 发明人:JEONG LAK SHIN 权利人:EWHA University—Industry Collaboration Foundation 摘要:The present invention relates to a fluoro-homoneplanocin A, its nucleoside derivative, and synthetic methods. The novel fluoro-homoneplanocin A and its nucleoside derivative in the present invention have an effect on cancer prevention or treatment, and therefore can be used as anticancer drugs.
参考文献:10.1007/s00784-020-03504-0 摘要:González-Serrano C, Phark JH, Fuentes MV, Albaladejo A, Sánchez-Monescillo A, Duarte S, Ceballos L. Effect of a single-component ceramic conditioner on shear bond strength of precoated brackets to different CAD/CAM materials. Clin Oral Investig. 2021 Apr;25(4):1953–65. doi: 10.1007/s00784-020-03504-0.