PROCESS FOR PREPARING 4-SUBSTITUTED-AMINO-3-CARBOXY OR CYANO-1,2-DIHYDRO-2-OXO-1,8-NAPHTHYRIDINE

摘要

Aminonaphthyridinones I (R1=H, alkyl, cycloalkyl, alkenyl, alkynyl; R2=cyano, COOH, alkoxycarbonyl, CONHNH2, carbamoyl; R3, R4=H, optionally substituted alkyl, acyl; NR3R4=heterocyclyl; R5, R6=H, alkyl, halo, alkylamino, alkoxy)were prepd. Thus, 7.14g 2-aminonicotionitrile was treated with 28.8g CH2(CO2Et)2 to give 2.9g I (R1=R3-R6=H, R2=CO2Et) which at 32mg/kg orally gave 68% inhibition of stomach acid secretion.