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
PROCESS FOR THE PREPARATION OF SOFOSBUVIR
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, (2017/06/09)
A process for the preparation of intermediates 9, useful in the synthesis of sofosbuvir, as well as intermediates of formula [12] are disclosed herein.
Method for preparing (2'R)-2'-deoxy-2-fluoro-2-methyluridine
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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
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Paragraph 0037, (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
IMPROVED PROCESSES FOR THE PREPARATION OF SOFOSBUVIR AND INTERMEDIATES THEREOF
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Paragraph 00140, (2016/12/22)
The present disclosure provides new procedures and intermediates for the preparation of Sofosbuvir.
A general and enantioselective approach to pentoses: A rapid synthesis of PSI-6130, the nucleoside core of sofosbuvir
Peifer, Manuel,Berger, Rapha?lle,Shurtleff, Valerie W.,Conrad, Jay C.,Macmillan, David W. C.
, p. 5900 - 5903 (2014/05/20)
An efficient route towards biologically relevant pentose derivatives is described. The de novo synthetic strategy features an enantioselective α-oxidation reaction enabled by a chiral amine in conjunction with copper(II) catalysis. A subsequent Mukaiyama aldol coupling allows for the incorporation of a wide array of modular two-carbon fragments. Lactone intermediates accessed via this route provide a useful platform for elaboration, as demonstrated by the preparation of a variety of C-nucleosides and fluorinated pentoses. Finally, this work has facilitated expedient syntheses of pharmaceutically active compounds currently in clinical use.