Copper-Catalyzed Electrophilic Amination of Heteroarenes and Arenes by CH Zincation†
Stacey L. McDonald
Department of Chemistry, Duke University, Durham, NC 27708-0346 (USA)
Search for more papers by this authorCharles E. Hendrick
Department of Chemistry, Duke University, Durham, NC 27708-0346 (USA)
Search for more papers by this authorCorresponding Author
Prof. Dr. Qiu Wang
Department of Chemistry, Duke University, Durham, NC 27708-0346 (USA)
Department of Chemistry, Duke University, Durham, NC 27708-0346 (USA)===Search for more papers by this authorStacey L. McDonald
Department of Chemistry, Duke University, Durham, NC 27708-0346 (USA)
Search for more papers by this authorCharles E. Hendrick
Department of Chemistry, Duke University, Durham, NC 27708-0346 (USA)
Search for more papers by this authorCorresponding Author
Prof. Dr. Qiu Wang
Department of Chemistry, Duke University, Durham, NC 27708-0346 (USA)
Department of Chemistry, Duke University, Durham, NC 27708-0346 (USA)===Search for more papers by this authorWe acknowledge financial support from Duke University and fellowships from the Burroughs Wellcome Endowment (S.L.M.) and the Duke University Pharmacological Sciences Training Program (C.E.H.).
Abstract
Direct amination of heteroarenes and arenes has been achieved in a one-pot CH zincation/copper-catalyzed electrophilic amination procedure. This amination method provides an efficient and rapid approach to access a diverse range of heteroaromatic and aromatic amines including those previously inaccessible using CH amination methods. The mild reaction conditions and good functional-group compatibility demonstrate its great potential for the synthesis of important and complex amines.
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