Chemistry - A European Journal · 2015 · 186 citations · 82 references
Natural SciencesChemistryMedicinal ChemistryCatalysisOrganic ChemistrySynthetic Medicinal ChemistryAntiviral AgentsAntiviral PharmacologyLate-stage FunctionalizationOrganic SynthesisCobalt CatalysisLate-stage Functionalization Via Cross-couplingMedicinal Chemistry ApplicationsOrganometallic CatalysisSubstrate ScopeSubstrate Scope ExpansionTransition Metal-catalyzed Synthesis
A cationic cobalt(III)-catalyzed direct C-H amidation of unactivated (hetero)arenes and alkenes by using 1,4,2-dioxazol-5-ones as the amidating reagent has been developed. This transformation proceeds efficiently under external oxidant-free conditions with a broad substrate scope. Moreover, 6-arylpurine compounds, which often exhibit high potency in antimycobacterial, cytostatic, and anti-HCV activities, can be smoothly amidated, thus offering a mild protocol for their late stage functionalization.
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