In order to examine biological activities, synthesis of 6-amino-2 (1H)-pyridones and their cyclization were carried out. The reaction of 4-cyano-3-butenoic acid esters (IIIa, b) with ammonia, methylamine, hydroxylamine, and hydrazine gave 6-amino-2 (1H)-pyridones (IVa, b) and the derivatives of IV having substituents such as methyl group (IVc), hydroxyl group (VII), or amino group (X) respectively, at 1-position. Condensation of these 1, 6-disubstituted 2 (1H)-pyridones with 1, 3-dicabonyl compounds or carboxylic acids resulted in the formation of 1, 8-naphthyridinone (VI), oxadiazolo [2, 3-a] pyridones (IX), or triazolo [2, 3-a] pyridones (XI).
