专利号:US-9845299-B2 优先权日:2013-01-14 标 题 :Process for the preparation of a fluorolacton derivative 发明人:CHEN RONGMIN; LI YUANQIANG; ZHAO JIANQIANG; ZHENG JIANBING; ZHU GUOLIANG 权利人:GILEAD PHARMASSET LLC 摘要:A novel process for the preparation of a fluorolactone derivative of the formula n n n n n n n n n n n n and of its acylated derivative of formula n n n n n n n n n n n n n n n n wherein R 1 stands for a hydroxy protecting group is described. n n n n n The acylated fluor lactones of formula V, particularly the benzoyl derivative with R 1 =benzyl are important precursors for the synthesis of prodrug compounds which have the potential to be potent inhibitors of the Hepatitis C Virus (HCV) NS5B polymerase.
专利号:US-9045520-B2 优先权日:2008-12-23 标题:Synthesis of purine nucleosides 发明人:CHUN BYOUNG-KWON; DU JINFA; RACHAKONDA SUGUNA; ROSS BRUCE; SOFIA MICHAEL JOSEPH; PAMULAPATI GANAPATI REDDY; CHANG WONSUK; ZHANG HAI-REN; NAGARATHNAM DHANPALAN 权利人:CHUN BYOUNG-KWON; DU JINFA; RACHAKONDA SUGUNA; ROSS BRUCE; SOFIA MICHAEL JOSEPH; PAMULAPATI GANAPATI REDDY; CHANG WONSUK; ZHANG HAI-REN; NAGARATHNAM DHANPALAN; GILEAD PHARMASSET LLC 摘要:A process for preparing phosphoramidate prodrugs or cyclic phosphate prodrugs of nucleoside derivatives, which is a compound, its stereoisomers, salts (acid or basic addition salts), hydrates, solvates, or crystalline forms thereof.
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-8716263-B2 优先权日:2008-12-23 标 题:Synthesis of purine nucleosides
专利号:US-2012316327-A1 优先权日:2008-12-23 标题 :Synthesis of purine nucleosides
专利号:US-2010279973-A1 优先权日:2008-12-23 标 题:Synthesis of purine nucleosides