Publication | Closed Access
Gold-Catalyzed 1,2-Aminoarylation of Alkenes with External Amines
88
Citations
51
References
2021
Year
Medicinal ChemistryCross-coupling ReactionDerivativesEngineeringAlkene MetathesisNatural SciencesDiversity-oriented SynthesisAminoarylation ProductsOrganic ChemistryCatalysisExternal AmineChemistryExternal AminesPharmacologyAsymmetric CatalysisCoupling PartnerBiomolecular Engineering
Reported herein is the gold-catalyzed 1,2-aminoarylation of alkenes that engages external amine as a coupling partner. Careful optimization studies revealed a significant role of the concentration of base to achieve highly chemoselective access to the aminoarylation products over potential C–N cross-coupled products. Overcoming all the limitations, the current strategy provided straightforward access to the medicinally relevant 3-aminochroman, 2-aminotetrahydronaphthalene, and 2-aminoindane derivatives.
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