| 摘要 |
<p>NEW MATERIAL:The compound of formula I [R<1> is lower alkyl or (F- substituted) phenyl; R<2> is H or lower alkyl; X is N or C-Y (Y is H, halogen, methyl or methoxy)]. EXAMPLE:1-Cyclopropyl-6,8-difluoro-1,4-dihydro-7-(trans-2-oxa-5,8- diazabicyclo[4,3,0]nonan-8-yl)-4-oxo-3-quinolinecarboxylic acid. USE:An antibacterial agent against Gram-positive bacteria, Gram-negative bacteria, etc. PREPARATION:A compound of formula II (R<3> is H or carboxyl-protecting group; Z is eliminable group) or its salt is made to react with a compound of formula III (R<20> is H, amino-protecting group or lower alkyl) usually in an inert solvent such as ethanol preferably at 80-150 deg.C for 1-6hr and, a necessary, removing the protecting group from the resultant compound of formula IV.</p> |
