| 摘要 |
PROBLEM TO BE SOLVED: To obtain the new derivative having a strong antimicrobial activity, remarkably improved in selective toxicity, useful as a medicine, an animal medicine, a marine medicine or an antimicrobial preservative, and high in safety. SOLUTION: An N1-(1,2-cis-2-halogenocyclopropyl)-substituted pyridone carboxylic acid derivative of formula I [R<1> is H, (substituted) amino or the like; R<2> is a substituent of formula II (R<3> -R<6> are each H, a 1-6C alkyl); A is C-X<3> (X<3> is a halogen, a 1-6C alkyl or the like), N; X<1> , X<2> are each a halogen; Z is H, a 1-6C alkyl or the like]. For example, 7-[3-(S)-amino-1-pyrrolidinyl]-6- fluoro-1-(1,2-cis-2-fluorocyclopropyl)-4-oxo-1,4-dihydroquinoline-3-ca rboxylic acid. The compound of formula I is obtained by hydrolyzing a compound of formula III and subsequently reacting the obtained free carboxylic acid derivative with a cyclic amine of the formula: R-H (R is the protected product of R<2> or the same cyclic amine of R<2> ). |
