Organic Letters · 2012 · 134 citations · 48 references
Natural SciencesChemistryMedicinal ChemistryOrganic ChemistryOrganometallic ChemistrySynthetic Medicinal ChemistryChemical BondingHeterocycle SynthesisMolecular BondingAccessArylation ReactionsC - H Bond FunctionalizationTransition-metal-catalyzed Heterocycle Synthesis
A C-H arylation with aryl chloride is made viable through a transition-metal-free approach. In the presence of a simple diol associating with KOt-Bu, various phenanthridine derivatives can be conveniently accessed. In particular, only 10 mol % of simple and inexpensive ethylene glycol is required for this protocol. These results represent the first general examples of aryl chloride/C-H coupling under transition-metal-free conditions.
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