Room temperature, copper-catalyzed amination of bromonaphthyridines with aqueous ammonia

Article abstract of DOI:10.1021/jo100476x

(Figure Presented) 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.