Process for preparing rifaximin

A preparation process and a rifaximin technology, applied in the field of rifaximin synthesis process, can solve the problems of high consumption of raw materials and energy, low production efficiency, large human injury, etc., so as to reduce treatment costs, protect the environment and save energy. energy effect

Active Publication Date: 2009-11-25
重庆赛诺生物药业股份有限公司
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, due to the use of highly toxic dichloromethane as a reaction solvent, the operating environment is more harmful to the human body, and the discharged dichloromethane pollutes the environment; Sodium sulfate drying, vacuum concentration to produce crude products and other processes (such as figure 2 As shown), the process is complicated, the production efficiency is low, and the consumption of raw materials and energy is large, and the cost is high

Method used

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  • Process for preparing rifaximin
  • Process for preparing rifaximin
  • Process for preparing rifaximin

Examples

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Embodiment 1

[0031] figure 1 For the preparation process flow chart of the present invention, in a 1000ml three-necked round-bottomed flask equipped with an electric stirrer, a thermometer and a reflux device, 400ml of ethanol was added, and 75.4g (0.1mol) of rifamycin O and 27g ( 0.25mol) 2-amino-4-methylpyridine, the temperature was raised to 40°C, and the reaction was stirred for 24 hours. After the reaction is completed, add 12.5g (0.09mol) of anhydrous potassium carbonate, stir for 30 minutes, filter, add 170ml of deionized water to the filtrate, crystallize, filter, and dry the filter cake to obtain 70.1g of rifaximin finished product, melting point: 200 ~205°C (decomposition), yield 89%.

Embodiment 2

[0033] The reaction vessel was the same as in Example 1, 500 ml of ethanol was added, 75.4 g (0.1 mol) of rifamycin O and 21.6 g (0.2 mol) of 2-amino-4-picoline were added successively under stirring, and the temperature was raised to 45 ° C and stirred. The reaction was carried out for 20 hours. After the reaction was completed, 13.8 g (0.1 mol) of anhydrous potassium carbonate was added, stirred for 30 minutes, filtered, and 180 ml of deionized water was added to the filtrate for crystallization to obtain 68.5 g of finished rifaximin with a yield of 87%.

Embodiment 3

[0035] The preparation process is the same as in Example 1, except that the addition of 2-amino-4-methylpyridine is 32.4g (0.3mol), and after the reaction is completed, 15.2g (0.11mol) of anhydrous potassium carbonate is added, and finally rife is obtained. The finished product of Ximing was 69.3 g, and the yield was 88%.

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Abstract

The invention discloses a process for preparing rifaximin, which comprises the following steps: fortimicin O is reacted with excessive 2-amino-4-picolyl for 20-24 hours at 35-45 DEG C by using ethanol as a reaction solvent; after the reaction, anhydrous potassium carbonate is added, wherein the mole number of the added anhydrous potassium carbonate is 0.9-1.1 times of that of the fortimicin O; the obtained mixture is stirred and filtered, and deionized water is added to obtained filter liquor for crystallizing; obtained filter mass is filtered; and after the filter mass is dried, a finished rifaximin product is obtained. The invention has the advantages of short time of the preparation process, simple and convenient post treatment, environmental protection, low consumption, high yield and low cost.

Description

technical field [0001] The invention relates to a process for chemically synthesizing drugs, in particular to a process for synthesizing rifaximin. Background technique [0002] Rifaximin, chemical name: 4-deoxy-4'-methylpyrido[1',2'-1,2]imidazo[5,4-C]rifaximin, the structural formula is as follows: [0003] [0004] Rifaximin is the first non-aminoglycoside potent and highly selective intestinal antibiotic, which has strong antibacterial effect and broad antibacterial spectrum. C. difficile, Staphylococcus epidermidis, Streptococcus faecalis, and Bacteroides spp. among the lanai anaerobes are highly active, while aminoglycoside antibiotics are basically inactive against these genera. In addition, this product also has good activity or high activity against Salmonella, Escherichia coli, Shigella, Yersinia enterocolitica, etc. Mainly used for infectious diarrhea, comprehensive diarrhea, hepatic encephalopathy (portal shunt), preventive treatment of postoperative infectio...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D498/22A61P31/00
Inventor 刘承悉白智权王廷彬李翔宇李洪
Owner 重庆赛诺生物药业股份有限公司
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