| 摘要 |
PROBLEM TO BE SOLVED: To obtain in high yield and purity on a practical production scale the subject compound having excellent antibacterial activity by reacting a specific amino group-protected aminopyrrolidine derivative with a specific quinolinecarboxylic acid derivative after protecting its amino group and thereafter deprotection. SOLUTION: This compound of formula V is obtained by the following process: the 5-position amino group of a compound of formula I is protected and the compound is converted to a compound of formula III [R1 is an acyl, (substituted) alkoxycarbonyl or the like] (e.g. 5-acetylamino-1-cyclopropyl-6,7- difluoro-1,4-dihydro-8-methyl-4-oxoquinoline-3-carboxylic acid), and thereafter, the compound of formula II is reacted with a compound shown by formula III [R2 is an acyl, (substituted) aralkyloxycarbonyl or the like; R3 and R4 are each H, methyl or the like] with its 3-position amino group protected e.g. (S)-7-tert-butoxycarnbonylamino-5-azaspiro [2.4]heptane} to obtain a compound of formula IV, and thereafter, the compound of formula IV is deprotected.
|
