PURPOSE: To obtain a new quinolonecarboxylic acid compound, having powerful antimicrobial action on Gram-negative and Gram-positive bacteria as an antimicrobial agent, excellent in absorbability by oral administration and having low toxicity.
CONSTITUTION: A compound expressed by formula I (R1 is cyclopropyl, 2fluoroethyl, etc.; R2 is hydroxymethyl, cyano, etc.; R3 and R4 are H, alkyl, etc.; X1 is H or halogen, provided that R2 is not cyano when R1 is cyclopropyl and X1 is H) and its salt, e.g. 1-cyclopropyl-6,8-difluoro-1,4-dihydro-7-(2- hydroxymethylmorpholino)-4-oxoquinoline-3-carboxylic acid. The aforementioned compound is obtained by carrying out condensing reaction of a compound expressed by formula II (X2 is halogen) with a compound expressed by formula III in a molar amount of 1-8 times based on the compound expressed by formula II at 30-150°C for 1-48hr.
| JP3037980 | [Title of Invention] Benzopyran derivative |
| WO/2015/050505 | BICYCLIC ALKYNE DERIVATIVES AND USES THEREOF |
KURODA TAKESHI
UEMORI SATORU
MORIGUCHI AKIHIKO
IKEDA TAKASHI
JAPAN TOBACCO INC
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