94695-49-5Relevant academic research and scientific papers
Structure of diethyl (polyfluorobenzoyl)malonates and their thermal intramolecular cyclization
Bazhin,Schegol'Kov,Kudyakova,Burgart,Saloutin
, p. 929 - 932 (2011)
The reaction of the C-ethoxymagnesium derivative of diethyl malonate with polyfluorobenzoyl chlorides affords the corresponding (polyfluorobenzoyl) malonates prone to thermal cyclization into coumarin derivatives. The compounds obtained are inherent in ke
Features of synthesis and structure of ethyl (2Z)-3-hydroxy-(2,3,4,5- tetrafluorophenyl)-propyl-2-enoate
Bazhin,Shchegol'kov,Kudyakova,Scherbakov,Burgart,Saloutin
experimental part, p. 116 - 121 (2012/06/04)
The structure of key intermediates in the synthesis of fluoroquinolone antibiotics: diethyl (2,3,4,5-tetrafluorobenzoyl)malonate and ethyl (2Z)-3-hydroxy-(2,3,4,5-tetrafluorophenyl)prop-2-enoate was for first time studied using X-ray diffraction (XRD) and
AN IMPROVED PROCESS FOR THE PREPARATION OF LEVOFLOXACIN HEMIHYDRATE
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Page/Page column 15-16, (2008/06/13)
The present invention relates to an improved process for preparation of Levofloxacin hemihydrate having single individual impurity not more than 0.1% and free from particulate matter and from the other enantiomer (R-form) which comprises dissolving levofloxacin technical grade in aqueous alkaline solution, treating the resulting solution with activated carbon at room temperature, removing the undissolved particulate matter filtration, bringing the pH of the aqueous alkaline levofloxacin solution to neutral using dilute mineral acid, removing the precipitated particulate matter by filtration, acidifying the resulting solution, treating the acidified solution with activated carbon at room temperature, filtering the undissolved particulate matter by filtration, neutralizing the acidic solution, filtering again to remove any particulate matter present and, extracting the resulting product with chlorinated solvent and concentrating under vacuum using aqueous tetrahydrofuran or in admixture with other organic solvents to get highly pure levofloxacin hemihydrate having single individual impurity is less than 0.1% and fee from particulate matter and from the other enantiomer (R-form).
Novel heterocyclic antibacterial compounds
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, (2008/06/13)
The invention provides heterocyclic organic compounds that inhibit bacterial DNA polymerase IIIC and type II bacterial topoisomerase. The invention further provides compounds that are useful as intermediates in the synthesis of such heterocyclic organic compounds. Syntheses and uses of such heterocyclic organic molecules are also described.
Cycloaracylation of Enamines, I. - Synthesis of 4-Quinolone-3-carboxylic Acids
Grohe, Klaus,Heitzer, Helmut
, p. 29 - 37 (2007/10/02)
Starting with o-halobenzoyl chlorides 4 and open-chain secondary enamines 5, a new synthesis of 4-quinolone-3-carboxylic acids 12 is described.The reaction of 7-haloquinolone-3-carboxylic acids 12a-k with aliphatic amines 14 produces highly active antibacterial 7-aminoquinolone-3-carboxylic acids 15.The main product of the 1-cyclopropyl series, "ciprofloxacin" (15a), is being developed as a broad-spectrum chemotherapeutic agent.
Antimicrobial 1-substituted phenyl-4-oxoquinoline-3-carboxylic acid compounds and compositions thereof
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, (2008/06/13)
Novel 1-substituted phenyl-4-oxoquinoline-3-carboxylic acid compounds of the formula: STR1 wherein R is hydrogen atom or fluorine atom, R° is hydroxy, fluorine atom or an alkanoyloxy having 1 to 6 carbon atoms, and X1 is hydrogen atom or fluorine atom, and a pharmaceutically acceptable salt thereof, said compounds having excellent antimicrobial activity and hence being useful as an antimicrobial agent, and a pharmaceutical composition comprising as an active ingredient said 1-substituted phenyl-4-oxoquinoline-3-carboxylic acid compounds or a pharmaceutically acceptable salt thereof in admixture with a pharmaceutically acceptable diluent or carrier.
Antibacterial 1,7-diamino-1,4-dihydro-4-oxo-3-quinolinecarboxylic acids
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, (2008/06/13)
Antibacterially effective 1,7-diamino-1,4-dihydro-4-oxo-3-(aza)quinolinecarboxylic acids of the formula STR1 in which A is nitrogen or C--R1, R1 is nitro or halogen, R2 and R3 each independently is C1
1-cyclopropyl-6-fluoro-1,4-dihydro-4-oxo-7-(3-oxo-1-piperazinyl)-3-quinolinecarboxylic acid antibacterial agents
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, (2008/06/13)
Novel antibacterially active 1-cyclopropyl-6-fluoro-1,4-dihydro-4-oxo-7-(3-oxo-1-piperazinyl)-3-quinolinecarboxylic acids of the formula STR1 in which R1 is hydrogen, methyl or ethyl, and R2 is hydrogen or fluorine, and pharmaceutically tolerable hydrates and salts thereof.
7-(3-aryl-1-piperazinyl)- and 7-(3-cyclohexyl-1-piperazinyl)-3-quinolonecarboxylic acid antibacterials
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, (2008/06/13)
Novel 1-cyclopropyl-4-fluoro-1,4-dihydro-4-oxo-7-(1-piperazinyl)-3-quinolinecarboxylic acid antibacterials of the formula STR1 in which R1 is hydrogen, alkyl with 1 to 4 carbon atoms and optionally substituted by hydroxyl, methoxy, amino, dimethylamino, halogen, cyano or alkoxycarbonyl having 1 or 2 carbon atoms in the alkyl moiety, or is oxoalkyl having up to 4 carbon atoms, phenacyl, or acyl having 1 to 4 carbon atoms, phenacyl, or acyl having 1 to 4 carbon atoms, R2 is phenyl or cyclohexyl optionally substituted up to three times by halogen, methyl, phenyl, cyano, hydroxyl, methoxy, benzyloxy, amino, methylamino, dimethylamino, piperidino or nitro, or is methylenedioxyphenyl, methylenedioxycyclohexyl, furyl, tetrahydrofuryl or thienyl, and X1 is hydrogen or fluorine, or pharmaceutically ultizable hydrates, acid addition salts, alkali metal salts or alkaline earth metal salts thereof.
