100986-89-8Relevant articles and documents
Novel ofloxacin derivatives: Synthesis, antimycobacterial and toxicological evaluation
Dinakaran, Murugesan,Senthilkumar, Palaniappan,Yogeeswari, Perumal,China, Arnab,Nagaraja, Valakunja,Sriram, Dharmarajan
, p. 1229 - 1236 (2008)
Thirty novel 9-fluoro-2,3-dihydro-8,10-(mono/di-sub)-3-methyl-8-nitro-7-oxo-7H-[1,4]oxazino[2,3,4-ij]quinoline-6-carboxylic acids were synthesized from 2,3,4,5-tetrafluoro benzoic acid and evaluated for in vitro and in vivo antimycobacterial activities against Mycobacterium tuberculosis H37Rv (MTB), multi-drug resistant Mycobacterium tuberculosis (MDR-TB), and Mycobacterium smegmatis (MC2) and also tested for the ability to inhibit the supercoiling activity of DNA gyrase from mycobacteria. Among the synthesized compounds, 10-[2-carboxy-5,6-dihydroimidazo[1,2-a]pyrazin-7(8H)-yl]-9-fluoro-2,3-dihydro-3-methyl-8-nitro-7-oxo-7H-[1,4]oxazino[2,3,4-ij]quinoline-6-carboxylic acid was found to be the most active compound in vitro with MIC99 of 0.19 μM and 0.09 μM against MTB and MTR-TB, respectively. In the in vivo animal model also the same compound decreased the bacterial load in lung and spleen tissues with 1.91 and 2.91 - log 10 protections, respectively, at the dose of 50 mg/kg body weight. Compound 10-[(4-((4-chlorophenyl)(phenyl)methyl)piperazin-1-yl)]-9-fluoro-2,3-dihydro-3-methyl-8-nitro-7-oxo-7H-[1,4]oxazino[2,3,4-ij]quinoline-6-carboxylic acid was found to be the most active in the inhibition of the supercoiling activity of DNA gyrase with an IC50 of 10.0 μg/mL. The results demonstrate the potential and importance of developing new oxazino quinolone derivatives against mycobacterial infections.
Synthesis method of levofloxacin carboxylic acid (by machine translation)
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, (2020/02/27)
The method comprises the following steps, mixing: dimethylaminopropyl methacrylate with an acid-binding agent in an organic solvent A, and then carrying out an amine exchange reaction A, to obtain N,N -tetrafluorobenzoyl - 3 3 3 3 3-dimethylaminopropyl A acrylate as shown in formula III B, in the reaction mixture A to obtain a mixture liquid, and a mixed solution 2 - (2, 3, 4, 5) - condensation reaction A; to obtain the compound. A. The reaction liquid L - is dissolved in an organic solvent, The reaction solution 2 - (2, 3, 4, 5) - is obtained by a condensation reaction with a mixture solution.) - The method comprises the following steps, (II). The method comprises the following steps of: adding B aminopropanol, to the reaction solution; and HCl, HOAc, H carrying out an amine exchange reaction with a mixed solution of N- propyl methyl acrylate. 2 The reaction of the acid system of O to give the levofloxacin carboxylic acid. of formula V prevents the preparation N,N - dimethylaminoethyl acrylate from being unstable and difficult, unsafe and expensive sodium ethoxide, to corrosion of the device. (by machine translation)
Environment-friendly method for preparing levofloxacin hydrochloride
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Paragraph 0019; 0023; 0027, (2017/10/05)
The invention provides an environment-friendly method for preparing levofloxacin hydrochloride. The method comprises the following steps: preparing 3-(2-hydroxy-1-methyl-ethylamino)-2-(2,3,4,5-tetrafluorobenzoyl)-ethyl acrylate, preparing levo-oxy main naphthenic acid, and preparing the levofloxacin hydrochloride. The method provided by the invention is concise, low in production cost, high in product yield, good in quality, economic and environment-friendly, fewer three wastes are discharged, and most byproducts are effectively separated and recycled, so that the method is convenient for industrial production and has great popularization significance.