AbstractWe demonstrate a unique strategy for a benzylation/benzylic CH amidation cascade reaction by the (η3‐benzyl)palladium system derived from a palladium catalyst and benzyl alcohol. This tandem process is devised as a new synthetic route for 3‐phenyl‐3,4‐dihydro‐(2H)‐1,2,4‐benzothiadiazine‐1,1‐dioxide. Water plays an important role for the smooth generation of the (η3‐benzyl)palladium species, and a bis‐benzylated Pd(II) intermediate would be formed in our catalytic system. Atom economical processes such as benzylic CH activation, cascade reactions and chemoselective reactions in aqueous media have been developed.magnified image
Compounds having the formula
1
are hepatitis C (HCV) polymerase inhibitors. Also disclosed are a composition and method for inhibiting hepatitis C (HCV) polymerase, processes for making the compounds, and synthetic intermediates employed in the processes.
The present invention provides an HCV polymerase inhibiting compound having the formula (I) and a composition comprising a therapeutically effective amount of said compound. The present invention also provides a method for inhibiting hepatitis C virus (HCV) polymerase, a method for inhibiting HCV viral replication, and a method for treating or preventing HCV infection. Processes for making said compounds, and synthetic intermediates employed in said processes, are also provided.
<i>N</i>-Benzylation/Benzylic CH Amidation Cascade by the (η<sup>3</sup>-Benzyl)palladium System in Aqueous Media: An Effective Pathway for the Direct Construction of 3-Phenyl-3,4-dihydro- (2<i>H</i>)-1,2,4-benzothiadiazine 1,1-Dioxides
AbstractWe demonstrate a unique strategy for a benzylation/benzylic CH amidation cascade reaction by the (η3‐benzyl)palladium system derived from a palladium catalyst and benzyl alcohol. This tandem process is devised as a new synthetic route for 3‐phenyl‐3,4‐dihydro‐(2H)‐1,2,4‐benzothiadiazine‐1,1‐dioxide. Water plays an important role for the smooth generation of the (η3‐benzyl)palladium species, and a bis‐benzylated Pd(II) intermediate would be formed in our catalytic system. Atom economical processes such as benzylic CH activation, cascade reactions and chemoselective reactions in aqueous media have been developed.magnified image