112811-67-3

Upstream product

• 112811-66-2 2,4,5-trifluoro-3-methoxybenzoyl chloride 
• 105-53-3 diethyl malonate 
• 2414-98-4 magnesium ethylate 
• 37892-24-3 potassium diethyl malonate 
• 112811-65-1 3-methoxy-2,4,5-trifluorobenzoic acid 
• 112811-64-0 2,4,5-trifluoro-3-methoxy-benzamide 
• 112811-63-9 3-methoxy-2,4,5-trifluorobenzonitrile 
• 13332-24-6 1-bromo-3-methoxy-2,4,5-trifluorobenzene 

Downstream Products

• 364069-19-2 ethyl 6,7-difluoro-1-[(1R,2S)-2-fluorocyclopropyl]-8-methoxy-4-oxo-1,4-dihydroquinoline-3-carboxylate 
• 122375-85-3 ethyl 3-ethoxy-2-(2,4,5-trifluoro-3-methoxybenzoyl)acrylate 
• 112811-70-8 ethyl 3-(cyclopropylamino)-2-(2,4,5-trifluoro-3-methoxybenzoyl)acrylate 
• 112811-60-6 1-Cyclopropyl-6-fluoro-8-methoxy-7-(3-amino-1-pyrrolidinyl)-1,4-dihydro-4-oxoquinoline-3-carboxylic acid 
• 146981-09-1 5-amino-7-(3-amino-1-pyrrolidinyl)-1-cyclopropyl-6-fluoro-1,4-dihydro-8-methoxy-4-oxo-3-quinolinecarboxylic acid 
• 112811-71-9 ethyl 8-methoxy-1-cyclopropyl-6,7-difluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylate 
• 160738-57-8 gatifloxacin 
• 112811-72-0 1-cyclopropyl-6,7-difluoro-1,4-dihydro-8-methoxy-4-oxo-3-quinolinecarboxylic acid 
• 112811-75-3 1-cyclopropyl-6-fluoro-1,4-dihydro-8-methoxy-7-(3-methylaminomethyl-1-pyrrolidinyl)-4-oxo-3-quinolinecarboxylic acid 
• 112811-68-4 ethyl 3-methoxy-2,4,5-trifluorobenzoylacetate 

Relevant academic research and scientific papers

Synthesis, antimycobacterial and antibacterial evaluation of l-[(1R, 2S)-2-fluorocyclopropyl]fluoroquinolone derivatives containing an oxime functional moiety

A series of novel 1-[(1R, 2S)-2-fluorocyclopropyl]fluoroquinolone derivatives 9aed containing an oxime functional moiety were synthesized and evaluated for their biological activity. Our results reveal that 9a1 and 9b3 have good in vitro activity against MTB H37Rv ATCC 27294 (MIC: 0.25 mg/mL) and two MDR-MTB clinical isolates (MICs: 0.065-0.125 mg/mL). Most of 9aed show potent activity against Escherichia coli and Klebsiella pneumoniae (MICs: 50s: 11.43-26.04 mg/kg).

Synthesis and evaluation of 1-cyclopropyl-2-thioalkyl-8-methoxy fluoroquinolones

Novel fluoroquinolone derivatives substituted with a 2-thioalkyl moiety, with and without a concomitant 3-carboxylate group, were synthesized to evaluate the effect of C-2 thioalkyl substituents on gyrase binding and inhibition. The presence of a 2-thioalkyl group universally decreased activity as compared to parent fluoroquinolones. However, with derivatives of moxifloxacin the presence of either a 2-thioalkyl group or a 3-carboxylate moiety increased activity over the 2,3-unsubstituted derivative. Energy minimization of structures provides an explanation for relative activities of fluoroquinolones having a C-2 thio moiety.

PROCESS FOR PRODUCING QUINOLONECARBOXYLIC ACID DERIVATIVE

Through a production process according to the following reaction scheme, compounds (2) which are useful for antibacterial agents can be provided at low cost and high yield.

Quinoline-3-carboxylic acid derivatives

Compounds of formula (I): STR1 (in which R1 is alkoxy, R is alkyl, haloalkyl, alkylamino, cycloalkyl or optionally substituted phenyl, X is chlorine or fluorine and Y is selected from certain specific heterocycles) have excellent antibacterial activity. They may be prepared by introducing the group represented by Y into the corresponding compound in which Y is replaced by a halogen atom.

8-alkoxyquinolonecarboxylic acid and salts thereof

Quinolonecarboxylic acid derivatives of the following formula: STR1 wherein R indicates a hydrogen atom or lower alkyl group, R1 indicates a lower alkyl group, R2 indicates a hydrogen atom, amino group or nitro group, X indicates a halogen atom, and Z indicates a halogen atom, piperazino group, N-methylpiperazino group, 3-methylpiperazino group, 3-hydroxypyrrolidino group, or pyrrolidino group of the following formula, STR2 (here, n is 0 or 1, R3 indicates a hydrogen atom or lower alkyl group, R4 indicates a hydrogen atom, lower alkyl group and R5 indicates a hydrogen atom, lower alkyl group, acyl group or alkoxycarbonyl group), the hydrates and pharmaceutically acceptable salts thereof are useful as antibacterial agents.