Efficient Pd-Catalyzed Amination of Heteroaryl Halides

Mark D. Charles, Phillip Schultz, and Stephen L. Buchwald*
Department of Chemistry, Massachusetts Institute of Technology, Cambridge, Massachusetts 02139
Org. Lett., 2005, 7 (18), pp 3965–3968
DOI: 10.1021/ol0514754
Publication Date (Web): August 10, 2005
Copyright © 2005 American Chemical Society
*

In papers with more than one author, the asterisk indicates the name of the author to whom inquiries about the paper should be addressed.

, sbuchwal@mit.edu

Abstract

Abstract Image

The Pd-catalyzed amination of a variety of heteroaryl halides has been accomplished by utilizing bulky electron-rich biaryl phosphine ligands. In particular, we report the first couplings of amines with chloro- and bromoindoles bearing a free NH, as well as the first Pd-catalyzed aminations of a 5-halopyrimidine.

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History

  • Published In Issue September 01, 2005
  • Received June 23, 2005

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