Publication | Closed Access
A Highly Convergent and Efficient Synthesis of a Macrocyclic Hepatitis C Virus Protease Inhibitor BI 201302
31
Citations
17
References
2013
Year
Bioorganic Chemistry0.1-0.2 M ConcentrationEfficient SynthesisChemistryAntiviral DrugRu-catalyzed Ring-closing MetathesisMedicinal ChemistryViral HepatitisAntiviral Drug DevelopmentOrganometallic CatalysisBiochemistryHighly ConvergentCatalysisPractical MacrocyclizationAntiviral CompoundBiomolecular EngineeringAlkene MetathesisNatural SciencesAntiviral TherapyHepatitisMedicineSynthetic ChemistryDrug Discovery
A highly convergent large scale synthesis of a 15-membered macrocyclic hepatitis C virus (HCV) protease inhibitor BI 201302 was achieved, in which the key features are the practical macrocyclization by Ru-catalyzed ring-closing metathesis (0.1 mol % Grela catalyst, 0.1-0.2 M concentration) and the efficient sulfone-mediated SNAr reaction.
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