166734-83-4Relevant articles and documents
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.
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.
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%.