Ornidazole green synthetic method

Abstract

The invention discloses an ornidazole green synthetic method, which is characterized in that 2-methyl-5-nitroimidazole and chloropropylene oxide are taken as raw materials, ethyl acetate is taken as a solvent, macroporous acidic high-molecular resin is taken as a catalyst, chloropropylene oxide is catalyzed and is performed with ring opening, and is performed alkylation condensation with 2-methyl-5-nitroimidazole, the ornidazole crude product can be obtained by one step reaction, and a supernatant liquid obtained by centrifugal separation is an ornidazole condensation liquid; the supernatant liquid is separated to obtain a mother liquor containing a catalyst, the mother liquor containing the catalyst is activated, the catalyst can be reutilized; and the ornidazole condensation liquid is performed with the processes of distillation, residues decoloring, filtering crystallization and recentrifugation to obtain the ornidazole. The ornidazole green synthetic method has high catalytic efficiency, mild reaction and reduced cost, the preparation yield can be increased from 66% to 75%, and the environmental pollution of waste water containing aluminum salt can be avoided.

Description

technical field [0001] The invention relates to a green synthesis method of ornidazole. Background technique [0002] The chemical name of ornidazole is α-(chloromethyl)-2-methyl-5-1H-imidazole-1-ethanol, CAS registration number: 16773-42-5, and its chemical structure is as follows: [0003] [0004] Ornidazole is the latest generation of 5-nitroimidazole drugs, which has high-efficiency anti-anaerobic bacteria, anti-trichomonas and anti-amoeba activities. It was first listed in Germany by Roche in 1977. Ornidazole has a wide range of indications, long-lasting action, and less side effects of the drug, and its drug effect is obviously better than traditional 5-nitroimidazoles such as metronidazole and tinidazole. At present, ornidazole has become the drug of choice in many countries in the prevention of anaerobic infection and the treatment of amebiasis, trichomoniasis, and various vaginal inflammations. Based on the above reasons, the consumption of ornidazole raw mate...

AI Technical Summary

Problems solved by technology

[0014] This process uses an excess of AlCl 3 As a catalyst, AlCl 3 When encountering a trace amount of water, it will be hydrolyzed to form hydrochloric acid mist. The acid mist in the production site is not good for the occupational health of employees, and the trace amount of moisture in the reaction system will greatly reduce the yield.

The biggest defect of this method is that after the synthesis reaction is completed, a large amount of waste water containing high aluminum salts will be produced. After the waste water is neutralized, it will become a precipitate of aluminum hydroxide. For every ton of ornidazole produced, 1.8 tons of aluminum hydroxide solids will be produced. Waste, there is no good treatment method for such a large amount of hazardous solid waste, enterprises cannot maintain normal production due to solid waste problems, and pollute the environment

However, because this method has short steps and acceptable yields, in recent years, some production enterprises at home and abroad have ignored environmental protection and actually adopted this preparation method to produce ornidazole raw materials. Therefore, there is currently no stable ornidazole at home and abroad. The supplier of the azole raw material greatly restricts the research and application of the drug

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