| 摘要 |
<p>A 4-oxo-1,4-dihydronicotinic acid driv. of formula (I) and its salt are prepd. by dehydrogating a 4-oxo-1, 4, 5, 6tetrahydronicotinic acid driv. of formula (III) and opt. removing carboxyl protecting gp.. Prepn. of (I) comprises ring closing of formula (II) under heat to obtain its driv. of (III). In the formulas, R1 is H or carboxyl protecting gp.; R2 is substd. aryl gp.; R3 is haloalkyl gp., aminoalkyl gp., or (un) substd. alkenyl, aralkenyl, aralkadienyl, aralkinyl, heterocyclicalkyl, hetero cyclicalkenyl, aryl, cycloalkyl, cycloalkenyl, acyl, iminoalkyl, heterocyclic or bridged hydrocarbon gp.. (I) is esp. effective against gram-positive and gram-negative bacteria.</p> |
