Chemistry - An Asian Journal · 2017 · 31 citations · 67 references
PharmacyMedicinal ChemistryDrug DiscoveryOrganometallic ChemistrySynthetic Medicinal ChemistryMacrocycle SynthesisSafer Chemical SynthesisBenzimidazole ChemistryBenzimidazole SynthesisMild Reaction ConditionsSubstrate ScopeSubstrate Scope ProfilingSubstrate Scope Screening
An efficient rhodium-catalyzed direct C-H amidation of N-nitrosoanilines with 1,4,2-dioxazol-5-ones as amidating agents has been developed. This method featured mild reaction conditions, a wide substrate scope and satisfactory yields. Besides, the amidated products could be readily converted to pharmaceutically valuable 1,2-disubstituted benzimidazoles via an HCl-mediated deprotection/cyclization process in one pot.
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