4.8 Article

Palladium-Catalyzed Amination of Unprotected Five-Membered Heterocyclic Bromides

Journal

ORGANIC LETTERS
Volume 16, Issue 3, Pages 832-835

Publisher

AMER CHEMICAL SOC
DOI: 10.1021/ol4035947

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Funding

  1. National Institutes of Health [GM58160]
  2. Astellas Foundation for Research on Metabolic Disorders

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An efficient method for the palladium-catalyzed amination of unprotected bromoimidazoles and bromopyrazoles is presented. The transformation is facilitated by the use of our newly developed Pd precatalyst based on the bulky biarylphosphine ligand tBuBrettPhos (L4). The mild reaction conditions employed allow for the preparation of a broad scope of aminoimidazoles and aminopyrazoles in moderate to excellent yields.

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