166734-83-4Relevant academic research and scientific papers
Nitroimidazole derivative, preparation method and application thereof
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Paragraph 0013; 0039-0041, (2021/05/12)
The invention provides a nitroimidazole derivative as shown in a general formula I or a pharmaceutically acceptable salt, a solvent compound, a hydrate, a polymorphic substance, a deuterated substance and an isomer thereof. The invention also provides a pharmaceutical composition containing the compound and application of the pharmaceutical composition. The nitroimidazole derivative provided by the invention has excellent pharmacokinetic properties, and also has excellent antibacterial activity.
Novel chiral stationary phases based on 3,5-dimethyl phenylcarbamoylated β-cyclodextrin combining cinchona alkaloid moiety
Zhu, Lunan,Zhu, Junchen,Sun, Xiaotong,Wu, Yaling,Wang, Huiying,Cheng, Lingping,Shen, Jiawei,Ke, Yanxiong
, p. 1080 - 1090 (2020/05/25)
Novel chiral selectors based on 3,5-dimethyl phenylcarbamoylated β-cyclodextrin connecting quinine (QN) or quinidine (QD) moiety were synthesized and immobilized on silica gel. Their chromatographic performances were investigated by comparing to the 3,5-dimethyl phenylcarbamoylated β-cyclodextrin (β-CD) chiral stationary phase (CSP) and 9-O-(tert-butylcarbamoyl)-QN-based CSP (QN-AX). Fmoc-protected amino acids, chiral drug cloprostenol (which has been successfully employed in veterinary medicine), and neutral chiral analytes were evaluated on CSPs, and the results showed that the novel CSPs characterized as both enantioseparation capabilities of CD-based CSP and QN/QD-based CSPs have broader application range than β-CD-based CSP or QN/QD-based CSPs. It was found that QN/QD moieties play a dominant role in the overall enantioseparation process of Fmoc-amino acids accompanied by the synergistic effect of β-CD moiety, which lead to the different enantioseparation of β-CD-QN-based CSP and β-CD-QD-based CSP. Furthermore, new CSPs retain extraordinary enantioseparation of cyclodextrin-based CSP for some neutral analytes on normal phase and even exhibit better enantioseparation than the corresponding β-CD-based CSP for certain samples.
Preparation method of optically active ornidazole
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Paragraph 0023-0025, (2021/01/04)
The invention relates to the technical field of organic chemical synthesis, in particular to a preparation method of optically active ornidazole. According to the preparation method, 2-methyl-5-nitroimidazole and optically active epoxy chloropropane are used as raw materials, an acid solvent is used as a reaction solvent, Lewis acid is used as a catalyst, a reaction is carried out under the condition close to normal temperature, and then extraction is carried out to obtain the product. Compared with the traditional optically active ornidazole synthesis process, the preparation method has theadvantages that the use of aluminum trichloride is avoided, the pollution of aluminum salt to the environment is reduced, low-temperature control in the reaction process is not needed, the reaction conditions are mild and easy to control, the temperature control cost can be reduced, the types of solvents are fewer, the operation is simple, and the cost is lower; and the method is suitable for industrial production of optically active ornidazole.
Process for preparing 5-nitroimidazole medicine through catalysis of small organic molecules
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Paragraph 0035-0040; 0047-0050, (2020/08/09)
The invention provides a process for preparing a 5-nitroimidazole medicine through catalysis of small organic molecules. The preparation method comprises the following steps: 1) uniformly stirring andmixing 2-methyl-5-nitroimidazole, a solvent and a catalyst which is selected from 1-(3, 5-ditrifluoromethyl phenyl)-3-(2-dimethylamino-cyclohexyl)-thiourea, and 2) adding epoxy chloropropane or epoxypropane into a reaction system in the step 1), and reacting to obtain the 5-nitroimidazole medicine. According to the present invention, the 5-nitroimidazole medicine prepared by using the synthesisprocess has characteristics of low catalyst consumption, high catalytic activity, high reaction selectivity, high yield, easy catalyst recycling, and environmental protection.
Synthesis method of 5-nitroimidazole drugs
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Paragraph 0039; 0040; 0043-0050, (2020/04/06)
The invention provides a synthesis method of 5-nitroimidazole drugs. The synthesis method comprises the steps: A) mixing 2-Methyl-5-nitroimidazole, ethyl acetate and aluminum trichloride catalyst supported on macroporous resin to obtain a mixed system; B) dropwise adding epichlorohydrin or propylene oxide to the mixed system and reacting to obtain a 5-Nitroimidazole antimicrobial drug. The aluminum trichloride catalyst supported on resin is adopted, the high catalytic activity of aluminum trichloride is retained, the post-reaction treatment process is simplified, the catalyst can be separatedonly through simple filtration, and the catalyst can be recycled for 3-5 times and activity basically remains unchanged, thus greatly reducing the three wastes of the catalyst used in the traditionalprocess and reducing the energy consumption and cost. Meanwhile, the aluminum trichloride catalyst supported on the resin is adopted and the reaction temperature does not need low temperature reaction, thus saving more energy and improving the reaction yield which can reach 75% ~ 80%.
Nitroimidazole derivative, preparation method and applications thereof
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Paragraph 0139-0146, (2020/02/29)
The invention relates to a nitroimidazole derivative, a preparation method and applications thereof, wherein specifically the compound has a structure represented by a formula I, and various groups and various substituents are defined in the specification. The invention further discloses a preparation method of the compound and applications of the compound in prevention, relieve and/or treatment of diseases caused by anaerobic bacteria infection.
High-safety L-ornidazole injection and preparation method thereof
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Paragraph 0052; 0053; 0056; 0059; 0062, (2018/04/03)
The invention provides a high-safety L-ornidazole injection. The high-safety L-ornidazole injection comprises L-ornidazole and an isoosmotic regulator component, and is characterized by containing nitrate, wherein the nitrate content is not higher than 30mg/l. The L-ornidazole injection is high in safety and low in toxicity, and the clinical therapeutic effect of the L-ornidazole can be better played.
Novel nitroimidazole drug as well as preparation method and application of novel nitroimidazole drug
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Paragraph 0024, (2018/04/01)
The invention relates to a novel nitroimidazole compound as well as a preparation method and application of the novel nitroimidazole compound to medical science and specifically relates to a nitroimidazole compound as shown in a general formula (I), a preparation method of the nitroimidazole compound and a pharmaceutical composition containing the compound. The invention aims at synthesizing a novel compound of a series of nitroimidazole derivatives by modifying the structure of a nitroimidazole compound, the compound can be used for obviously reducing adverse reaction in clinic, meanwhile, the compound has a relatively ideal effect on protecting the liver and kidneys, and the clinical application of the compound is apparent.
S-ornidazole injection with high safety and preparation method thereof
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Paragraph 0051-0052, (2017/10/07)
The invention provides an s-ornidazole injection with high safety. The s-ornidazole injection is prepared from components of s-ornidazole and an isoosmotic adjusting agent; the s-ornidazole injection is characterized in that the s-ornidazole injection contains acetamide, wherein the content of the acetamide is not higher than 10 mg/l. The s-ornidazole injection provided by the invention is high in safety and low in toxicity, and is capable of well exerting the clinical effects of the s-ornidazole.
L-ornidazole α crystal and its preparation method (by machine translation)
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Paragraph 0030; 0031; 0032; 0033, (2016/11/28)
The invention belongs to the technical field of preparation of pharmaceutical forms, and, in particular relates to a crystalline α L-ornidazole and method for preparing the same. Crystalline α of the L-ornidazole, using cu-Kα radiation, in order to 2 the angle of the X-ray powder diffraction in 10.7 ±0 . 2 °, 14.3 ±0 . 2 °, 15.9 ±0 . 2 °, 18.0 ±0 . 2 °, 21.6 ±0 . 2 °, 22.2 ±0 . 2 °, 23.8 ±0 . 2 °, 24.7 ±0 . 2 °, 25.3 ±0 . 2 °, 28.8 ±0 . 2 °, 29.3 ±0 . 2° and 31.2 ±0 . 2° is displayed X-ray powder diffraction peak. Crystalline α L-ornidazole of this invention high purity, quality stability is good; the preparation method has a simple process, the solvent used for less harm to human body, safety, is suitable for industrial production. The invention yield is 80-90%, the product purity ≥ 99.9%. (by machine translation)
