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Discovery of ABT-267, a pan-genotypic inhibitor of HCV NS5A.
We describe here N-phenylpyrrolidine-based inhibitors of HCV NS5A with excellent potency, metabolic stability, and pharmacokinetics. Compounds with 2S,5S stereochemistry at the pyrrolidine ringExpand
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The total synthesis of (+)-dragmacidin F.
The first total synthesis of (+)-dragmacidin F has been accomplished, establishing the absolute configuration of this biologically important, antiviral marine alkaloid. The convergent route describedExpand
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Development of an enantiodivergent strategy for the total synthesis of (+)- and (-)-dragmacidin f from a single enantiomer of quinic Acid.
An enantiodivergent strategy for the total chemical synthesis of both (+)- and (-)-dragmacidin F beginning from a single enantiomer of quinic acid has been developed and successfully implemented.Expand
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The palladium-catalyzed aerobic kinetic resolution of secondary alcohols: reaction development, scope, and applications.
The first palladium-catalyzed enantioselective oxidation of secondary alcohols has been developed, utilizing the readily available diamine (-)-sparteine as a chiral ligand and molecular oxygen as theExpand
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The Resolution of Important Pharmaceutical Building Blocks by Palladium-Catalyzed Aerobic Oxidation of Secondary Alcohols
The palladium-catalyzed aerobic oxidative kinetic resolution of key pharmaceutical building blocks is described. Substrates investigated are relevant to the enantioselective preparation of Prozac ¾ ,Expand
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Heterogeneous reductive isomerization reaction using catalytic Pd/C and H2.
[reaction: see text] A highly selective catalytic reductive isomerization reaction is described. The extremely mild and neutral reaction conditions (10% Pd/C, H2, and MeOH at 0 degrees C) tolerate aExpand
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Kinetic Modeling of the Nickel-Catalyzed Esterification of Amides
Nickel-catalyzed coupling reactions provide exciting tools in chemical synthesis. However, most methodologies in this area require high catalyst loadings, which commonly range from 10-20 mol %Expand
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Quantitative Impurity Rejection Analysis for Crystallization
The analysis of impurity profiles is one of the most frequently performed activities in drug development. While mass-based quantification using a reference standard often provides the highest degreeExpand
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