- NITRATION
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The present invention relates to a process for preparing a nitrated compound, comprising the step of reacting a compound (A) comprising at least one substituted or unsubstituted aromatic or heteroaromatic ring, wherein said heteroaromatic ring comprises at least one heteroatom selected from the group consisting of oxygen, sulfur, phosphor, selenium and nitrogen, with a compound of formula (I) wherein Y is selected from the group consisting of hydrogen and nitro.
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Page/Page column 36; 44; 73
(2020/05/28)
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- Process for preparing 5-nitroimidazole medicine through catalysis of small organic molecules
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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.
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Paragraph 0041-0046; 0051-0052
(2020/08/09)
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- Synthesis method of 5-nitroimidazole drugs
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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%.
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Paragraph 0041; 0042; 0043; 0051; 0052
(2020/04/06)
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- Synthetic Secnidazole method and Secnidazole
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The invention discloses a method for synthesizing secnidazole and secnidazole. According to the method, 2-methyl-5-nitroimidazole and 1-bromine-2-propyl alcohol serve as raw materials, acetone serves as a solvent, and potassium carbonate or sodium carbonate serves as a catalyst. The method comprises the following steps: mixing 2-methyl-5-nitroimidazole, 1-bromine-2-propyl alcohol, the catalyst and acetone, carrying out a reflux reaction, and obtaining a reaction mixture A after the reaction is ended; separating and purifying the reaction mixture A, and obtaining the secnidazole. According to the method, 2-methyl-5-nitroimidazole and 1-bromine-2-propyl alcohol serve as the raw materials, acetone serves as the solvent, and the potassium carbonate or sodium carbonate serves as the catalyst, so that secnidazole is synthesized, strong acids are avoided, and the corrosion to the equipment and pipeline system is reduced. Moreover, the reaction temperature is low, and the reaction time is short, so that the energy consumption is reduced.
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Paragraph 0036-0042
(2016/10/07)
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- External preparation for skin diseases containing nitroimidazole
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An external preparation for skin disease which comprises a nitroimidazole derivative represented by the following formula (I): wherein R1, R3 and R4 may be the same or different and represent a hydrogen atom, a nitro group, a lower alkyl group, a substituted lower alkyl group, a lower alkenyl group, or a substituted lower alkenyl group; and R2 represents a hydrogen atom, a lower alkyl group, a substituted lower alkyl group and a lower alkenyl group or a substituted lower alkenyl group, provided that any one of R1, R3 and R4 is a nitro group.
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