| 摘要 |
<p>PURPOSE:To obtain a fluoroquinoline derivative useful as an antimicrobial agent showing excellent antimicrobial activity against both Gram-positive and Gram-negative bacteria, providing high concentration in blood by oral and parenteral administrations having low toxicity and high safety. CONSTITUTION:A fluoroquinoline derivative of formula 1 [R1 is H or lower alkyl; R2 is H, (protected)amino, (protected)aminocarbonyl or (protected)carboxyl; R5 is halogen, lower alkyl, (protected)OH or R2; R6 is lower alkyl; A is CH2, ((protected)N or O; (n) and (m) are 0-4 and n+m=1-4] such as 1-cyclopropyl-7- diphenylmethoxycarbonylmethyl-6-fluoro-8-methoxy-1,4-dihydro-4-oxo-3- quinolinecarboxylic acid ethyl ester. The compound of formula I such as a compound of formula 7 (R4 is carboxy-protecting group) is obtained by using a compound of formula 2 as a raw material and through a compound of formula 4 (R3 is R4) and a compound of formula 5.</p> |
