874638-98-9Relevant articles and documents
Discovery of Novel Nucleotide Prodrugs with Improved Potency Against HCV Variants Carrying NS5B S282T Mutation
Zhen, Le,Dai, Liang,Wen, Xiaoan,Yao, Lan,Jin, Xiaoliang,Yang, Xiao-Wen,Zhao, Wenfeng,Yu, Sheng-Qi,Yuan, Haoliang,Wang, Guangji,Sun, Hongbin
, p. 6077 - 6088 (2017)
Resistant HCV variants carrying NS5B S282T mutation confer reduced sensitivity to sofosbuvir, the sole marketed NS5B polymerase inhibitor. On the basis of the finding that 2′-α-F-2′-β-C-methylcytidine 5′-triphosphate (8) was more potent than sofosbuvir's
Method for preparing (2'R)-2'-deoxy-2-fluoro-2-methyluridine
-
Paragraph 0010; 0019; 0020, (2018/01/17)
The invention provides a method for preparing sofosbuvir intermediate (2'R)-2'-deoxy-2-fluoro-2-methyluridine (compound VII), which comprises the following steps: (1) enabling a compound I to react with lithium diisopropylamide in aprotic solvent serving as a reaction solvent, controlling the reaction temperature to 0-5 DEG C, and treating after the reaction is completed to obtain a compound X; and (2) enabling the compound X to react with an NaClO solution having a concentration of 6-10 percent in the existence of a phase transfer catalyst, keeping the reaction temperature to 20-30 DEG C, and treating after the reaction is completed, wherein the reaction solvent is the aprotic solvent. The method does not require column chromatography in post-treatment, has a yield reaching 8 percent, and is applicable to industrial production.
High-yield synthesis method of sofosbuvir and sofosbuvir prepared with method
-
, (2016/11/07)
The invention relates to a high-yield synthesis method of sofosbuvir and sofosbuvir prepared with the method. The method comprises steps as follows: (a) cytidine and benzoic anhydride are dissolved in a first organic solvent for a reaction; TIDPSCl2 is ad