Room Temperature, Copper-Catalyzed Amination of Bromonaphthyridines with Aqueous Ammonia

Room temperature, copper-catalyzed amination of amido-bromo-1,8-naphthyridines is reported. Use of Cu2O and aqueous ammonia at ambient temperature affords amination products in 10-87% yield. Bromonaphthyridines are prepared in 15-65% yield via treatment of amidonaphthyridinones with phosphorus tribromide. This methodology provides an alternative route to functional, nonsymmetric 2,7-diamido-1,8-naphthyridines.