Method for preparing imidazole antifungal medicine derivate

An antifungal drug and imidazole technology, which is applied in the field of preparation of imidazole antifungal drug derivatives, can solve the problems of high toxicity of raw materials and auxiliary materials, complicated reaction process, unfavorable large production, etc., and achieves improved market competitiveness, simple operation, The effect of less by-products

Inactive Publication Date: 2012-06-27
杭州欧拓普生物技术有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0011] This process route is long, the reaction process is complicated, and the raw materials used are relatively toxic, and the total yield is not high, about 85%, which is not conducive to large-scale industrial production

Method used

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  • Method for preparing imidazole antifungal medicine derivate
  • Method for preparing imidazole antifungal medicine derivate
  • Method for preparing imidazole antifungal medicine derivate

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] Add 10g of ketoconazole to a 500ml three-neck flask, add 100ml of 1mol / L NaOH solution, stir to mix evenly, add 50ml of absolute ethanol, and under the protection of nitrogen, heat the material to 50°C and react for 10 hours. After cooling the reaction material to room temperature, ice water was added to precipitate a solid, which was filtered and dried to obtain 2.7 g of a white solid. The content of the deacetylated product detected by HPLC was greater than 98%, and the yield was 29.2%.

Embodiment 2

[0033] Add 10g of ketoconazole to a 500ml three-neck flask, add 100ml of 1mol / L NaOH solution, stir to mix evenly, add 50ml of absolute ethanol, and under the protection of nitrogen, heat the material to 85°C and reflux for 4 hours. After the reaction material was cooled to room temperature, cold water was added to precipitate a solid. After filtration and drying, 8.7 g of a white solid was obtained. The content of deacetylated product was greater than 98% as detected by HPLC, and the yield was 94%.

Embodiment 3

[0035] Add 10g of ketoconazole to a 500ml three-neck flask, add 100ml of 1mol / L sodium carbonate solution, stir to mix evenly, add 5ml of triethylamine, heat to 90°C under the protection of nitrogen, and reflux for 4 hours. After the reaction material was cooled to room temperature, cold water was added to precipitate a solid, and 8.9 g of a white solid was obtained by filtration and drying. The content of the deacetylated product was greater than 98% as detected by HPLC, and the yield was 96.2%.

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Abstract

The invention discloses a method for preparing an imidazole antifungal medicine derivate, which is characterized by comprising the following steps of: (a) heating ketoconazole in an organic solvent in the existence of alkaline substances, and removing acetyl to obtain a deacetylated product; and (b) dissolving the deacetylated product in the organic solvent, slowly dropping diethyl pyrocarbonate in the existence of a condensing agent, and reacting to obtain the imidazole antifungal medicine derivate. The invention greatly improves the yield of the reaction product, greatly reduces the cost required by production as all reagents can be repeatedly used and enhances the market competitive capacity of the product. The invention also has the advantages of simple operation, less reaction steps,high purity, less by-products, good reaction stability, and the like, is suitable for industrialized production, also has greater application prospect and less pollution as concentrated hydrochloric acid is not used in the reaction process and is beneficial to environmental protection.

Description

technical field [0001] The invention relates to the field of drug synthesis, in particular to a preparation method of imidazole antifungal drug derivatives. Background technique [0002] Imidazole antifungal drug derivatives belong to a kind of imidazole antifungal drugs, and its structural formula is as follows: [0003] [0004] Imidazole antifungal drug derivatives are effective in treating aspergillosis, cryptococcosis, histoplasmosis, candidiasis, sporotrichosis, chromoblastomycosis and dermatophytosis (including tinea versicolor, etc.). Good curative effect, is an antifungal drug with high efficiency and low toxicity, which can be taken orally and externally. The application of imidazole antifungal drug derivatives in cosmetics and shampoos can regulate and control the secretion of skin oil, inhibit the growth of bacteria and fungi on the skin surface, and effectively control and improve the recurrence of acne and the generation of dandruff. [0005] The preparati...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D405/06A61P31/10A61Q17/00
Inventor 傅锦浩陈伟良
Owner 杭州欧拓普生物技术有限公司
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