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A treating method of a ganciclovir condensation compound isomer

A technology of ganciclovir condensate and processing method, which is applied in the field of chemical substance recovery to achieve the effects of reducing environmental pollution, reducing raw material cost and improving total yield

Active Publication Date: 2015-07-08
LIVZON GROUP CHANGZHOU KONY PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But because the accumulative amount of ganciclovir condensate isomers can be more and more, and the amount that adds ganciclovir condensate isomers in the condensation reaction system can not increase without limit, therefore, develop a kind of The processing method of the condensate isomer of ganciclovir is a problem to be studied at present

Method used

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Examples

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Effect test

Embodiment 1

[0031] Put 40g of ganciclovir condensate isomers, 2g of p-toluenesulfonic acid and 160ml of DMF into the reaction flask, add 5ml of acetic anhydride, and keep the reaction at 120-130°C for 45h. After the reaction, the solvent was concentrated under reduced pressure, and 320ml of methanol was added to dissolve the residue. After the solution was clear, it was cooled to 20-25°C, and stirred for 3h to crystallize. After filtering, the filtrate was concentrated under reduced pressure, and the concentrated residue was dissolved in a mixed solvent composed of 30ml of methanol and 170ml of toluene, and then cooled to 5-10°C for crystallization for 2h. Filter, add the filter cake to 200ml of methanol, stir at 50-60°C for 1 hour, cool to 5-15°C and stir for 1 hour. Filter and dry to obtain 20.8g of ganciclovir condensate, as attached figure 1 As shown, GCVM2 is an isomer of ganciclovir condensate, the purity of ganciclovir condensate is 99.136%, and the isomer content is 0.094%.

Embodiment 2

[0033] Put 40g of ganciclovir condensate isomers, 2g of p-toluenesulfonic acid and 160ml of DMSO into the reaction flask, add 5ml of acetic anhydride, and keep the reaction at 120-130°C for 45h. After the reaction, the solvent was concentrated under reduced pressure, and 320ml of methanol was added to dissolve the residue. After the solution was clear, it was cooled to 20-25°C, and stirred for 3h to crystallize. After filtering, the filtrate was concentrated under reduced pressure, and the concentrated residue was dissolved in a mixed solvent composed of 30ml of methanol and 170ml of toluene, and then cooled to 5-10°C for crystallization for 2h. Filter, add the filter cake to 200ml of methanol, stir at 50-60°C for 1 hour, cool to 5-15°C and stir for 1 hour. Filter and dry to obtain 19.8g of ganciclovir condensate, as attached figure 2 As shown, GCVM2 is an isomer of ganciclovir condensate, the purity of ganciclovir condensate is 99.057%, and the isomer content is 0.095%.

Embodiment 3

[0035] Put 40g of ganciclovir condensate isomers, 2g of p-toluenesulfonic acid and 160ml of formamide into the reaction flask, add 5ml of acetic anhydride, and keep the reaction at 120-130°C for 45h. After the reaction was completed, the solvent was concentrated under reduced pressure, and 320ml of methanol was added to dissolve the residue. After dissolving, cool to 20-25°C and stir for 3h to crystallize. After filtering, the filtrate was concentrated under reduced pressure, and the concentrated residue was dissolved in a mixed solvent composed of 30ml of methanol and 170ml of toluene, and then cooled to 5-10°C for crystallization for 2h. Filter, add the filter cake to 200ml of methanol, stir at 50-60°C for 1 hour, cool to 5-15°C and stir for 1 hour. Filter and dry to get ganciclovir condensate 20.2g, as attached image 3 As shown, GCVM2 is an isomer of ganciclovir condensate, the purity of ganciclovir condensate is 99.096%, and the isomer content is 0.217%.

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Abstract

The invention relates to the technical field of chemical compound recovery, and particularly relates to a method of converting a ganciclovir condensation compound isomer into a ganciclovir condensation compound. The method utilizes a characteristic that the ganciclovir condensation compound isomer can be converted into the ganciclovir condensation compound by structural transformation in a solution, and the ratio of the ganciclovir condensation compound isomer to the ganciclovir condensation compound in the solution is in a dynamic equilibrium relationship of about 35:65. By adoption of the technical scheme, the purity of the obtained ganciclovir condensation compound can be more than 98.0%, wherein the content of the ganciclovir condensation compound isomer is less than 0.5% and the yield is about 50%. The method effectively overcomes treatment problems of the ganciclovir condensation compound isomer, increases the total yield of the ganciclovir condensation compound, indirectly reduces the raw material cost of the ganciclovir condensation compound, reduces environment pollution and is suitable for popularization and application.

Description

technical field [0001] The invention relates to the technical field of chemical substance recovery, in particular to a method for converting ganciclovir condensate isomers into ganciclovir condensate. Background technique [0002] Ganciclovir is a nucleoside antiviral drug that can competitively inhibit DNA polymerase and incorporate into the DNA of viruses and host cells, thereby inhibiting DNA synthesis. The product was launched by the Syntex company of the United States and was approved for marketing in 1988. It is the drug of choice for the treatment of cytomegalovirus infection. In foreign countries, the indication of ganciclovir is the induction and maintenance treatment of immunodeficiency patients (including AIDS patients) complicated with cytomegalovirus retinitis, and it can also be used for the prevention of cytomegalovirus seropositive AIDS patients in patients receiving organ transplantation Prevention of cytomegalovirus disease. In addition to the prevention ...

Claims

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Application Information

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IPC IPC(8): C07D473/18
CPCC07D473/18
Inventor 陈敖卢兵孙永康马立新沈娟
Owner LIVZON GROUP CHANGZHOU KONY PHARMA
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