title: Palladium-catalyzed amination of aryl halides on solid support.
abstract: [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.
authors.affiliation: Novartis Research Institute, Brunner Strasse 59, A-1235 Vienna, Austria. klaus.weigand@pharma.novartis.com
authors.forename: Klaus
authors.initials: K
authors.lastname: Weigand
authors.forename: Sylvie
authors.initials: S
authors.lastname: Pelka