106648-05-9Relevant academic research and scientific papers
Chemical synthesis method for norfloxacin
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Paragraph 0029, (2018/04/01)
The invention discloses a chemical synthesis method for norfloxacin. The chemical synthesis method comprises the following steps: (1) synthesis of a compound ethyl quinolinate: 3-ethylamino-2-(2,4-dichloro-5-fluorobenzoyl) ethyl acrylate is dissolved in DMF, potassium carbonate is added, the mixture is heated to 50-80 DEG C, reacts and stands overnight, a product is cooled and poured into cold water, produced solids are filtered, solids are washed with a large amount of water, and the product ethyl quinolinate is obtained; (2) synthesis of a compound quinolinic acid: ethyl quinolinate is dissolved in methanol, hydrochloric acid is added in a ratio being 1:1, reflux is performed for 2 h, white solids are precipitated and filtered, a filter product is washed with water and dried in a vacuum oven for 2 h, and the product quinolinic acid is obtained. The design is reasonable, and one novel norfloxacin synthesis method is selected and has good market application value.
Intermediate synthetic method of carbostyril drug
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Paragraph 0011; 0013; 0015, (2018/04/01)
The invention discloses an intermediate synthetic method of a carbostyril drug. The method comprises the following steps: stirring a mixture of 3-dimethylamino ethyl acrylate and triethylamine at room temperature; adding a solution of 2,4-dichloro-5-fluorobenzoyl chloride through a charging funnel; stirring the mixture to react for 3 hours at 80-90 DEG C; filtering to form a mixture; washing a solid with methylbenzene; dissolving the washed solid with water; dropwise adding ethyl acetate to fully dissolve the solution; cooling the solution, and leaving the solution to stand to separate out a white solid; performing centrifugalization; and drying the solid for 2 hours to obtain a white solid. The method disclosed by the invention is reasonable in design, and the novel method of synthesizing 3-ethylamino-2-(2,4-dichloro-5-fluorobenzoyl) ethyl acrylate has a very good market application value.
A norfloxacin, ciprofloxacin and enrofloxacin preparation method
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Paragraph 0093-0094, (2017/04/25)
The invention discloses a preparation method of norfloxacin, ciprofloxacin and enrofloxacin. The preparation method comprises the following steps: directly reacting 1-ethyl-6-fluoro-7-chlo-4-oxo-1,4-dihydro-quinoline-3-carboxylate or 1-cyclopropyl-6-fluoro-7-chlo-4-oxo-1,4-dihydro-quinoline-3-carboxylate with piperazine (or N-ethyl piperazine); and then, performing after-treatment to prepare a corresponding target product norfloxacin (or ciprofloxacin or enrofloxacin). The preparation method disclosed by the invention is short in reaction step, convenient to operate, less investment and beneficial to industrial production; consumption of piperazine (or N-ethyl piperazine) can be reduced by more than half; under the catalytic action, the reaction temperature is low, the byproducts are less, the yield is high and the cost is low; heavy use of inorganic acid and inorganic alkaline is avoided, so that the pollution is reduced.
Cycloaracylation of Enamines, I. - Synthesis of 4-Quinolone-3-carboxylic Acids
Grohe, Klaus,Heitzer, Helmut
, p. 29 - 37 (2007/10/02)
Starting with o-halobenzoyl chlorides 4 and open-chain secondary enamines 5, a new synthesis of 4-quinolone-3-carboxylic acids 12 is described.The reaction of 7-haloquinolone-3-carboxylic acids 12a-k with aliphatic amines 14 produces highly active antibacterial 7-aminoquinolone-3-carboxylic acids 15.The main product of the 1-cyclopropyl series, "ciprofloxacin" (15a), is being developed as a broad-spectrum chemotherapeutic agent.
