Abstract An efficient approach is developed to prepare different 2-amino-1, 4- naphthalenedione and 6-amino-5, 8-quinolinedione derivatives regioselectively by Au (III)- catalyzed 1, 4-nucleophilic addition and subsequent oxidation. A wide variety of primary, secondary, and aromatic amines, as well as allylamine and 2-butynylamine are well tolerated under the mild conditions to give products in moderate to good yields.