A simple approach toward N(3)-substituted-2,3-diaminopyridines is presented, based on Pd-catalyzed C,N-cross coupling. The use of RuPhos- and BrettPhos-precatalysts in combination with LiHMDS allows for C,N-cross coupling reactions of unprotected 3-halo-2-aminopyridines with primary and secondary amines.
© 2011 American Chemical Society