Fenticonazole nitrate, preparation of levorotatory form and dextrorotatory form and application of levorotatory form in preparing antifungal medicaments
A fenticonazole nitrate and a reaction technology are applied in the preparation of fenticonazole nitrate levorotatory and dextrorotary forms, and the application in the preparation of antifungal drugs, in the field of antifungal action of fenticonazole nitrate and levorotatory forms, which can solve the problem of Cumbersome, affecting industrial application value, complex operation and other problems, to achieve the effect of high product content, improving industrial application value, and good industrial application value
Active Publication Date: 2012-10-31
NANJING HEALTHNICE MEDICAL TECH +1
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Problems solved by technology
[0005] The present invention provides a kind of synthetic technique of fenticonazole nitrate, and the yield is higher; The present invention also provides a kind of preparation method of fenticonazole nitrate L-isomer and D-isomer, which solves the complex operation, It is cumbersome and affects the problem of industrial application value; the present invention also demonstrates that the antifungal activity of L-fenticonazole nitrate is greater than that of racemate and D-isomer, and the L-isomer can be made into antifungal by adding excipients or carriers Drugs, which are available in oral formulations and topical formulations for skin application
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[0086] 1 Preparation of Fenticonazole Nitrate
[0087] Step 1, the preparation of copper phenylmercapto
[0088] 28.6g of cuprous oxide, 44g of thiophenol, and 500ml of ethanol were added to the reaction flask, heated to reflux and stirred for 3 hours, and the solvent was recovered under reduced pressure to obtain about 69g of the product. (yield 99%)
[0089] Step 2, the preparation of p-iodobenzoic acid
[0090] A. Add 260mL of 24% sulfuric acid and 13.7g of p-aminobenzoic acid into a 1000mL three-necked bottle, heat up and stir until all p-aminobenzoic acid is dissolved, let the solution cool down to 0-5°C. Slowly add 25 mL of 7.3 g of sodium nitrite solution dropwise, stir for 40 minutes to allow it to fully react, then add 0.6 g of urea, filter to obtain a diazonium salt solution, and store at low temperature.
[0091] B. Dissolve 17.5g of potassium iodide in 160mL of distilled water, raise the temperature at 40°C, keep the temperature constant, slowly add the diazoniu...
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The invention relates to a synthesis process for fenticonazole nitrate. In the synthesis process, thiophenol and para aminobenzoic acid are taken as raw materials, and are subjected to seven-step reaction to form the fenticonazole nitrate, and the yield is higher. The invention relates to a preparation method for a levorotatory form and a dextrorotatory form of the fenticonazole nitrate, which solves the problem that the levorotatory form and the dextrorotatory form cannot be well obtained due to complicated and fussy operation according to documents. The levorotatory form and the dextrorotatory form have high purity and high industrial application value. Experiments prove that the antibacterial activity of the levorotatory form of the fenticonazole nitrate is greater than that of racemate and the dextrorotatory form. The invention relates to application of the levorotatory form of the fenticonazole nitrate in preparing antifungal medicaments.
Description
technical field [0001] The invention relates to a synthesis process of fenticonazole nitrate and a preparation method of fenticonazole nitrate L-isomer and D-isomer. The invention also relates to the antifungal effect of fenticonazole nitrate L-body and its application in the preparation of antifungal medicine. Background technique [0002] Fenticonazole nitrate is a chiral broad-spectrum antifungal drug, which is effective against skin fungi, yeasts and other fungi that cause skin mycosis. It has bacteriostatic effect at low concentrations and bactericidal effect at high concentrations. The racemate of fenticonazole nitrate is currently clinically used for treatment. [0003] Current literature reports that the synthetic process yield of fenticonazole nitrate is relatively low, and the total yield is only 10%. [0004] It has been reported in the literature that fenticonazole nitrate was separated to obtain the L-isomer and the D-isomer by HPLC and capillary electrophores...
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IPC IPC(8): C07D233/60C07B57/00A61K31/4174A61P31/10
Inventor 邹巧根
Owner NANJING HEALTHNICE MEDICAL TECH