Relevant articles and documents
All total 30 Articles be found
Mechanism-Based Solution to the ProTide Synthesis Problem: Selective Access to Sofosbuvir, Acelarin, and INX-08189
Simmons, Bryon,Liu, Zhuqing,Klapars, Artis,Bellomo, Ana,Silverman, Steven M.
, p. 2218 - 2221 (2017)
A general and efficient method for the synthesis of pronucleotide (ProTide) 5'-phosphoramidate monoesters is reported. This method consists of a highly stereoselective 5'-phosphorylation mediated by dimethylaluminum chloride to afford the desired target ProTides in excellent yields without employing 3'-protection strategies. The application of this methodology to the synthesis of a number of pharmaceutically relevant compounds currently marketed or under investigation in clinical research is demonstrated.
Method for synthesizing Sofosbuvir
-
Paragraph 0030-0067, (2020/04/17)
The invention discloses a method for synthesizing Sofosbuvir. The method comprises the steps of adding a compound 1, a compound 2 and dichloromethane into a reaction bulb, cooling the temperature to 0DEG C, then, adding aluminum chloride, adding a proper amount of pyridine, and carrying out a reaction at a reaction temperature of 15 DEG C to 20 DEG C, thereby producing the Sofosbuvir. According to the method, the reaction is high in conversion ratio and good in regioselectivity and stereoselectivity, so that the synthesis cost of the Sofosbuvir is reduced, and the method has remarkable socialand economic benefits.
PROCESS FOR THE PREPARATION OF (Sp)-SOFOSBUVIR AND INTERMEDIATES THEREOF
-
Page/Page column 13; 14, (2018/03/28)
The present invention is directed towards process for preparation of an optically pure (Sp)-Sofosbuvir of Formula-(I) and its intermediate namely (Sp)-isomer of isopropyl alanyl phosphoramidate of Formula (III) thereof.