4.8 Article

Copper- Catalyzed Electrophilic Amination of Heteroarenes and Arenes by C-H Zincation**

Journal

ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
Volume 53, Issue 18, Pages 4667-4670

Publisher

WILEY-V C H VERLAG GMBH
DOI: 10.1002/anie.201311029

Keywords

amination; CH functionalization; copper; heterocycles; synthetic methods

Funding

  1. Duke University
  2. Burroughs Wellcome Endowment
  3. Duke University Pharmacological Sciences Training Program

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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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