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Method for synthesizing ketoconazole

A technology for synthesizing ketoconazole and a condensation reaction, which is applied in the field of raw material drug synthesis and synthesizing ketoconazole, can solve the problems of small batch size, high recovery difficulty and high cost, and achieves the advantages of saving production cost, shortening production cycle and improving production efficiency. Effect

Inactive Publication Date: 2015-03-25
NANJING BAIJINGYU PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] Purpose of the invention: To solve the problem of small batch size, heavy odor, large amount of solvent used in refining ketoconazole, difficult recovery and high cost in each batch

Method used

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  • Method for synthesizing ketoconazole
  • Method for synthesizing ketoconazole
  • Method for synthesizing ketoconazole

Examples

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Embodiment Construction

[0020] Add 300kg of ketoconazole water precipitate and 1200kg of ethanol into the refining kettle, and add 6kg of activated carbon, heat up and reflux for 30 minutes and then press into the crystallization kettle. After cooling down to 0-5°C with icy brine, centrifuge and filter for 40 minutes.

[0021]

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PUM

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Abstract

The invention relates to a method for synthesizing ketoconazole. The method is characterized in that the production process comprises the following steps: carrying out condensation reaction; elutriating; centrifuging; drying; refining; crystallizing; centrifugalizing; drying; granulating; crushing; mixing; internal packaging; external packaging; and warehousing, wherein in the refining step, ethanol is used as a refining solvent; in the refining process, active carbon is further added; and in the refining step, conventional ethyl acetate is replaced with ethanol as the refining solvent, and the refining batch is improved by 2.5 times (weight ratio) every batch, so that the production period is shortened, the production efficiency is improved and the production cost is lowered.

Description

technical field [0001] The invention relates to the field of synthesizing raw materials, in particular to the field of synthesizing ketoconazole. Background technique [0002] Ketoconazole is an imidazole antifungal drug, and its mechanism of action is to inhibit the biosynthesis of ergosterol in the fungal cell membrane, affect the permeability of the cell membrane, and inhibit its growth. It can be used to treat superficial and deep fungal diseases, such as skin and nail ringworm, vaginal candidiasis, gastrointestinal fungal infections, etc., as well as systemic infections caused by Candida albicans, Coccidioides, and Histoplasma. Its structural formula is: [0003] [0004] Its synthesis route is as follows: [0005] [0006] The ketoconazole production process mentioned in the present invention is condensation reaction, water analysis, centrifugation, drying, refining, centrifugation, drying, sizing, crushing, mixing, inner packaging, outer packaging and storage....

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D405/06
CPCC07D405/06
Inventor 冯佳佳陶月宝
Owner NANJING BAIJINGYU PHARMA
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