| 摘要 |
<p>PROBLEM TO BE SOLVED: To highly efficiently obtain a quinolone carboxylic acid derivative which is expected to be a quinolone carboxylic acid-based synthetic antimicrobial agent used for medicines, agrochemicals or the like, by reacting a specific quinolone carboxylic acid compound with a specified azaspiroheptane compound in a specified amount or more. SOLUTION: This method for producing a quinolone carboxylic acid derivative of formula III comprises reacting a compound of formula I [X is a releasing group; R1 is a (substituted) 3 to 6C cyclic alkyl; R2 is H or an amino-protecting group; R3 is H, phenyl, acetoxymethyl or the like] 5-amino-6,7-difluoro-1-[(2S)- fluoro-(1R)-cyclopropyl]-1,4-dihydro-8-methyl-4-oxoquinolone-3-carboxylic acid} with three or more equivalents of a compound of formula II [(n) is 1 to 5; R is H or an amino-protecting group] for example, (7S)-tertiary butoxycarbonylamino-5-azaspiro[2.4]heptane} preferably at 100 to 120 deg.C.</p> |
