Refining method for ganciclovir

A ganciclovir and refining method technology, applied in the field of chemical refining, can solve the problems of long refining cycle, high energy consumption, low yield and the like, and achieve the effects of short refining cycle, low energy consumption and high yield

Active Publication Date: 2012-08-08
LIVZON GROUP CHANGZHOU KONY PHARMA
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  • Abstract
  • Description
  • Claims
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AI Technical Summary

Problems solved by technology

[0005] Method 1. the guanine impurity content in the prepared ganciclovir is relatively high, generally reaching more than 5%, the method of reducing the guanine impurity content in the ganciclovir reported in the literature is: under heating condition, dissolve crude product with water more Ciclovir, then add a large amount of activated carbon to carry out adsorption treatment, cool and crystallize after hot filtration, filter, repeat the described hot water dissolving-activated carbon adsorption-cooling crystallization-filtration process, until qualified ganciclovir is obtained, about to repeat The above-mentioned operation is more than 8 times; the guanine impurity content in the ganciclovir prepared by method 2. is generally below 1%, and the qualified ganciclovir can be obtained through 3 to 5 times of the above-mentioned refining operations; the refining method in the prior art There are problems of long refining cycle, high energy consumption and low yield

Method used

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  • Refining method for ganciclovir

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0018] A kind of guanine content is the refining method of the 20g ganciclovir crude product of 3.68%, comprises the following steps:

[0019] (1) 300ml of 20% formic acid solution is used to drop into the reaction flask, the temperature is raised to reflux, and the reflux is maintained for 0.5 hour, the solid is not completely dissolved, and 1g of gac is added, and reflux is performed for 30 minutes, filtered, the filter cake is washed with hot water, drained, and the filtrate is combined, Refrigerate to crystallize;

[0020] (2) Suction filtration gained filtrate and crystallization mixture, get crystallization product with 100ml of 5% NaOH solution, dissolve and stir at room temperature for 1 hour, add 100ml of water for dilution, then adjust the system to neutral with dilute hydrochloric acid, stir and crystallize for 2 hours Afterwards, suction filtration, the crystalline product was washed and dried to obtain 15.7 g of ganciclovir, and the impurity guanine content was re...

Embodiment 2

[0022] A kind of guanine content is the refining method of the 20g ganciclovir crude product of 1.19%, comprises the following steps:

[0023] (1) Put 300ml of 15% formic acid solution into the reaction bottle, heat up to reflux, add 1g of activated carbon after the solid is fully dissolved, reflux for 30 minutes, filter, wash the filter cake with hot water, drain, wash the filtrate and combine, put in the refrigerator to refrigerate and crystallize;

[0024] (2) Suction filtration gained filtrate and crystallization mixture, get crystallization product with 100ml of 5% NaOH solution, dissolve and stir at room temperature for 1 hour, add 100ml of water for dilution, then adjust the system to neutral with dilute hydrochloric acid, stir and crystallize for 2 hours Afterwards, suction filtration, the crystalline product was washed and dried to obtain 16.1 g of ganciclovir, and the impurity guanine content was reduced to 0.22%.

Embodiment 3

[0026] A kind of guanine content is the refining method of the 20g ganciclovir crude product of 1.19%, comprises the following steps:

[0027] (1) Put 300ml of 15% glacial acetic acid solution into the reaction bottle, heat up to reflux, add 1g of activated carbon after the solid is fully dissolved, reflux for 30 minutes, filter, wash the filter cake with hot water, drain, combine the washing filtrates, and refrigerate to crystallize ;

[0028] (2) Suction filtration gained filtrate and crystallization mixture, get crystallization product with 100ml of 5% NaOH solution, dissolve and stir at room temperature for 1 hour, add 100ml of water for dilution, then adjust the system to neutral with dilute hydrochloric acid, stir and crystallize for 2 hours Afterwards, suction filtration, the crystalline product was washed and dried to obtain 16.3 g of ganciclovir, and the impurity guanine content was reduced to 0.42%.

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Abstract

The invention relates to the technical field of chemical refining, in particular to a refining method for ganciclovir. The refining method specifically comprises the following steps of: heating to dissolve the ganciclovir by using lower fatty acid aqueous solution; filtering off insoluble substances therein; cooling, crystallizing and suction-filtering filtrate; treating through inorganic alkali solution and then adjusting to be neutral, wherein the content of guanine impurity in the ganciclovir is reduced by a method of obtaining solid through crystallization. According to the method of reducing the content of the guanine impurity in the ganciclovir adopted in the refining method, the content of the guanine impurity can be reduced to be below 0.50 percent; and the method has the advantages of no need of repeating crystallization operation, short refining period, low energy consumption and high yield and is suitable for large-scale industrial production.

Description

technical field [0001] The invention relates to the technical field of chemical refining, in particular to a refining method of ganciclovir. Background technique [0002] The chemical name of ganciclovir is 9-(1,3-dihydroxy-2-propoxymethyl)-guanine, which is a nucleoside antiviral drug that can competitively inhibit DNA polymerase and incorporate into viruses and host cells DNA, inhibits DNA synthesis. Ganciclovir is a derivative of acyclovir, which is more effective than acyclovir, has a wider antiviral spectrum, has a highly specific effect on cytomegalovirus, and has a stronger inhibitory effect on human cytomegalovirus than acyclovir It has a certain effect on herpes simplex virus type I and type II, varicella zoster virus, Epstein-Barr virus, etc. This product was launched by Syntex Company of the United States and was approved for marketing in 1988. It is the first choice drug for the treatment of cytomegalovirus infection. [0003] The synthetic method of ganciclovi...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D473/18
Inventor 陈敖俞军陈争一李鸣海
Owner LIVZON GROUP CHANGZHOU KONY PHARMA
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