Palladium-catalyzed amination of aryl halides on solid support.
[reaction: see text] The first examples of the Pd(0)-catalyzed amination of aryl halides using Rink-resins as nitrogen source are described. Pd(2)dba(3)/BINAP/NaO-t-Bu was found to be the most efficient catalyst/base system, while a solvent mixture of dioxane and tert-butyl alcohol was shown to enhance the selectivity toward the desired monoarylation. Moderate to good yields and excellent purities of the amination products were found with electron-poor aryl halides, while electon-rich aryl halides failed to react under these conditions.
Weigand
Klaus
K
Novartis Research Institute, Brunner Strasse 59, A-1235 Vienna, Austria. klaus.weigand@pharma.novartis.com
Pelka
Sylvie
S