| abstract |
NEW MATERIAL:A compound of formula I [R 1 is H or a protecting group of the carboxyl group; R 2 is substituted aryl or (substituted) heterocyclic group; R 3 is aralkenyl, aralkadienyl, aralkynyl, aryl, heterocyclic ring-alkenyl or heterocyclic group which may have a substituent group] and a salt thereof. n EXAMPLE: 6-(4-Aminophenyl)-1-(4-fluorophenyl)4-oxo-1,4-dihydronicotinic acid. n USE: An antimicrobial agent, capable of acting effectively on Gram-positive and Gram-negative bacteria, and exhibiting powerful antimicrobial action particularly on germs resistant to antibiotic substances. n PROCESS: A compound of formula II (R 7 is a protecting group of the carboxyl group) obtained by subjecting a compound of the formula R 3 CHO as a raw material to the Wittig reaction is reacted with methyl orthoformate and When with an amine of the formula R 2 NH to give a compound of formula III, which is then cyclized and reduced to afford a compound of formula V(the compound of formula I in which R 1 is R 7 ). The resultant compound of formula V is then hydrolyzed to give the aimed compound of formula I (R 1 is H). n COPYRIGHT: (C)1984,JPO&Japio |