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Room-Temperature Palladium-Catalyzed Coupling of Heteroaryl Amines with Aryl or Heteroaryl Bromides
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2012
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Room TemperatureRoom-temperature Palladium-catalyzed CouplingCross-coupling ReactionEngineeringEnantioselective SynthesisOrganic ChemistryOrganometallic CatalysisCatalysisStereoselective SynthesisChemistryHeteroaryl BromidesAsymmetric CatalysisAttractive Biaryl AminesHeteroaryl AminesBiomolecular Engineering
Heteroaryl amines readily undergo Buchwald-Hartwig amination reactions with a range of aryl and heteroaryl bromides at room temperature using t-BuXPhos Pd-precatalyst and NaOt-Bu. The pharmaceutically attractive biaryl amines are generally formed in short reaction times (0.5-16 h) and in good to excellent yields.