4887-24-5Relevant articles and documents
Preparation method of moxifloxacin hydrochloride chelate
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Paragraph 0021; 0027-0032, (2021/03/05)
The invention provides a preparation method of moxifloxacin hydrochloride chelate, and belongs to the technical field of heterocyclic compound preparation. The preparation method comprises the following steps: keeping excessive acetic acid, adding trimethyl borate into the acetic acid, and reacting at 110-120 DEG C; after the reaction is finished, cooling, adding gatifloxacin intermediate, heatingto 110-120 DEG C after the addition is finished, keeping on reacting; recovering the fraction under reduced pressure until the reaction is finished, and recovering the solvent until the solvent is dry to obtain the chelate. The method has the advantages of simple process, economy, environmental friendliness and high product purity.
Synthesis, photophysical and solvatochromic properties of diacetoxyboron complexes with curcumin derivatives
Lyu, Heng,Wang, Dan,Cai, Lian,Wang, Dun-Jia,Li, Xiao-Ming
, (2019/06/03)
Five novel diacetoxyboron complexes of β-diketones incorporated curcumin moiety were designed and synthesized. Their photophysical behaviors were investigated by UV–vis absorption and fluorescence spectroscopy in different solvents and solid state. It was observed that their fluorescence spectra yielded a blue to yellow-green emission in solution and emitted a yellow to red emission in solid state. Especially, the complex 3b displayed the strongest emission and the highest quantum efficiency (Φu = 0.98) in toluene among these complexes. The CIE coordinate of the complex 3b in solid state was positioned in an ideal red region of the chromaticity diagram. The maximal emission of these complexes exhibited a large wavelength shift and Stokes shift increased with the increase of the solvent polarity. Their dipole moment differences between the ground and excited states were also estimated by using the Lippert–Mataga equation. Meanwhile, their HOMO, LUMO energy levels and energy band gaps were calculated by cyclic voltammetry.
Preparation method of moxifloxacin hydrochloride
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Paragraph 0018-0028; 0031-0041; 0044-0054, (2019/08/30)
The invention discloses a preparation method of moxifloxacin hydrochloride. The method comprises the following steps: performing condensation by using 1-cyclopropyl-6,7-difluoro-1,4-dihydro-8-methoxy-4-oxo-ethylquinolinecarboxylate as a central ring, and (S,S)-2,8-diazabicyclo[4,3,0]nonane as a side chain, after alkali hydrolysis is completed, adding a part of 6N hydrochloric acid, performing primary crystallization, adding the remaining 6N hydrochloric acid, performing secondary crystallization, and performing recrystallization on the crystallized product obtain by the secondary crystallization once by using ethanol to obtain the moxifloxacin hydrochloride with a high content and excellent quality. When the method provided by the invention is adopted to prepare the moxifloxacin hydrochloride, product loss caused by repeated crystallization is reduced, labor intensity is reduced, energy consumption is reduced, product stability is improved, product quality is greatly improved, and themethod is suitable for industrialized large-scale production; and the prepared moxifloxacin hydrochloride contains 99.6%-102.0% of C21H25ClFN3O4 calculated by an anhydrate, and has a low total impurity content.
Preparation method of Zabofloxacin
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Paragraph 0035-0046, (2018/10/19)
The invention provides a preparation method of Zabofloxacin. The preparation method comprises the following steps of after the reaction on main ring chelates shown as a formula I and a side chain shown as a formula II in a non-protonic solvent, removing chelation parts; generating midbodies shown as a formula III; removing protection groups from the midbodies shown as the formula III; generating the Zabofloxacin. The Zabofloxacin prepared by the technical path does not need to be further purified; the yield is high; the purity is high; the method is suitable for industrial production.
SOLID PHARMACEUTICAL COMPOSITION
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Paragraph 0096, (2016/04/20)
[Problem] To provide a solid pharmaceutical composition which contains a compound represented by general formula (1) or a salt thereof and suppresses decomposition of said compound or salt thereof, and a production method of said solid pharmaceutical composition. [Solution] This solid pharmaceutical composition contains a compound represented by general formula (1) or a salt thereof, a cellulosic excipient, and an acidic substance of pH 4.0 or less.
Synthesis of Bicyclic Boron Heterocycles Containing [1,3,4,2]Oxadiazaborole and [1,3,2]Oxazaborine
Kotali, Antigoni,Maniadaki, Anna,Kotali, Elvira,Harris, Philip A.,Rózycka-Soko?owska, Ewa,Ba?czewski, Piotr,Joule, John A.
, p. 4117 - 4125 (2016/11/26)
Boron triacetate, generated in situ, reacts with various 3-(2-acylhydrazono)-2-(2-phenylhydrazono)butanoic acids to give 4-acetoxy-2-aryl-8-methyl-6-oxo-7-phenylhydrazono-2H,4H,6H,7H,8H-[1,3,4,2]oxadiazaborolo[2,3-b][1,3,2]oxazaborines in good yields. These derivatives represent a class of new zwitterionic, tetrahedral boron heterocycles. X-ray single-crystal analyses of one of the starting (acylhydrazono)butanoic acids as well as of one heterocyclic boron product are reported.
SOLID PHARMACEUTICAL COMPOSITION
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Paragraph 0103-0110, (2016/04/09)
[Problem] To provide a novel pharmaceutical composition which contains a medically active component and which can suppress delays in the release of said component due to gelling. [Solution] This solid pharmaceutical composition contains a compound represented by general formula (1), or a salt thereof, a cellulosic excipient, and a salting-out agent.
Method for producing oxyborate Tetracyanobicyclo
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Paragraph 0042, (2016/12/16)
PROBLEM TO BE SOLVED: To provide a method for producing a tetracyanoborate compound safely and efficiently from an inexpensive raw material. SOLUTION: In the method for producing a tetracyanoborate salt, a boron compound represented by general formula (1): B-(X-Y-R)3(wherein, X represents S or O, Y represents CO or SO2, R represents a 1-10C hydrocarbon group, a halogenated hydrocarbon group, or a halogen, each of X, Y and R may be identical to or different from one another, and two or more Rs may be connected with each other), and a cyano compound are made to react with each other. COPYRIGHT: (C)2013,JPOandINPIT
Synthesis of novel dehydroacetic acid N-aroylhydrazone-derived boron heterocycles
Kotali, Antigoni,Dimoulaki, Fani,Kotali, Elvira,Maniadaki, Anna,Harris, Philip A.,Rózycka-Soko?owska, Ewa,Ba?czewski, Piotr,Joule, John A.
, p. 7245 - 7249 (2015/08/24)
Abstract The synthesis of new boron heterocycles is reported via the reaction of dehydroacetic acid N-aroylhydrazones with boron acetate. The procedure involves formation of new zwitterionic, tetrahedral boron structures.
Synthesis and crystal structure of 1-cyclopropyl-6,7-difluoro-8-methoxy-4- oxo-1,4-dihydro-3-quinoline carboxylic acid-(O3,O4)-bis-(acetate-O)borate
Li, Fei,Zhang, Jie,Jiang, Yu,Jin, Lei,Zhang, Chuan
, p. 6079 - 6082 (2013/07/26)
The crystal structure of the 1-cyclopropyl-6,7-difluoro-8-methoxy-4-oxo-1, 4-dihydro-3-quinoline carboxylic acid-(O3,O4)-bis-(acetate-O)borate has been determined by single crystal X-ray diffraction method. The crystal belongs to monoclinic with space group P2(1)/n, with a = 16.818(9), b = 6.585(4), c = 18.663(4)?, a = 90, b = 107.351(7), g = 90, V = 1972.8(18)?3, Z = 4, Dx = 1.479 Mg/m3, l(MoKa) = 0.128, F(000) = 908, ?(MoKa) = 0.128 mm-1, R = 0.1083 and wR = 0.3062 for 2378 reflections with I > 2s(I). The two rings of fluoroquinolone and borate ring are almost coplanar with dihedral angles values lower than 2. The crystal structure is stabilized by intermolecular hydrogen bonds and p-p stacking interactions.