| 摘要 |
<p>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. EXAMPLE:6-(4-Aminophenyl)-1-(4-fluorophenyl)4-oxo-1,4-dihydronicotinic acid. 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. 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).</p> |
