Water-Mediated Catalyst Preactivation for Efficient Pd-Catalyzed
Aminations

B. P. Fors; P. Krattiger; E. Strieter; S. L. Buchwald

doi:10.1055/s-0028-1083461

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Synfacts 2008(11): 1206-1206
DOI: 10.1055/s-0028-1083461

Metal-Mediated Synthesis

Water-Mediated Catalyst Preactivation for Efficient Pd-Catalyzed Aminations

Contributor(s): Paul Knochel, Tobias Thaler
B. P. Fors, P. Krattiger, E. Strieter, S. L. Buchwald*
Massachusetts Institute of Technology, Cambridge, USA

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Publication History

Publication Date:
23 October 2008 (online)

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Significance

A new efficient protocol for Pd-catalyzed amination reactions is described in this article. Preactivation of the Pd(OAc)₂-biaryldialkylphosphine catalyst system with water leads to shorter reaction times, avoids the use of additives, such as BEt₃, and allows lower catalyst loadings in couplings of amides and anilines with aryl chlorides.