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Ganciclovir sodium synthesis process

A technology of ganciclovir sodium and synthesis process, applied in the field of medicine, can solve problems such as in-depth research on the preparation of ganciclovir sodium, and achieve the effects of easy industrial production, shortening reaction time, and improving product purity and yield

Pending Publication Date: 2021-09-07
HAINAN HAILING CHEMIPHARMA CORP
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] The "Synthetic Process Improvement of Ganciclovir" written by Liu Xinyuan, which was recorded in the fifth issue of "Chemical Design Communication" in 2017, disclosed that diacetylguanine was used as a starting material to prepare ganciclovir sodium salt. Instead of refining triacetyl ganciclovir, prepare the method for obtaining ganciclovir again, the purpose of this method is to prepare ganciclovir, ganciclovir sodium exists as an intermediate, and the ganciclovir sodium does not preparation for in-depth study

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] A kind of synthetic technique of ganciclovir sodium, comprises the following steps:

[0027] S1. Mix 100g of diacetylguanine and 1.6g of p-toluenesulfonic acid, then add 600mL of N,N-dimethylformamide-methanol solution, heat to 105°C, add 110mL of triacetylmethoxyglycerin and 25g The adsorbent was heated to 175°C at a rate of 12°C / min, stirred and reacted at a rate of 45r / min for 5h, concentrated under reduced pressure, evaporated to dryness, washed with water, ethyl acetate, methanol and evaporated to dryness, and methanol was taken The washing liquid was dried to obtain 118.2 g triacetylganciclovir;

[0028] The N,N-dimethylformamide-methanol solution is obtained by mixing N,N-dimethylformamide and methanol at a volume ratio of 1:2.2;

[0029] The adsorbent is obtained by mixing zeolite molecular sieve and HPD-600 resin in a weight ratio of 1:0.5;

[0030] S2. Ethanol and water are mixed according to the volume ratio of 2:1, then add the sodium hydroxide of ethanol ...

Embodiment 2

[0032] A kind of synthetic technique of ganciclovir sodium, comprises the following steps:

[0033] S1. Mix 100g of diacetylguanine and 1g of p-toluenesulfonic acid, then add 500mL of N,N-dimethylformamide-methanol solution, heat to 100°C, put in 100mL of triacetylmethoxyglycerin and 22g of adsorption and then heated to 165°C at a rate of 10°C / min, stirred and reacted at a rate of 40r / min for 6h, concentrated under reduced pressure and evaporated to dryness, washed with water, ethyl acetate, methanol and evaporated to dryness, and the washed methanol The liquid was dried to obtain 119.5g triacetylganciclovir;

[0034] The N,N-dimethylformamide-methanol solution is obtained by mixing N,N-dimethylformamide and methanol at a volume ratio of 1:2;

[0035] The adsorbent is obtained by mixing zeolite molecular sieve and HPD-600 resin in a weight ratio of 1:0.46;

[0036] S2. Ethanol and water are mixed according to the volume ratio of 1:1, then add the sodium hydroxide of ethanol ...

Embodiment 3

[0038] A kind of synthetic technique of ganciclovir sodium, comprises the following steps:

[0039] S1. Mix 100g of diacetylguanine and 2g of p-toluenesulfonic acid, then add 800mL of N,N-dimethylformamide-methanol solution, heat to 120°C, put in 120mL of triacetylmethoxyglycerol and 35g of adsorption and then heated to 178°C at a rate of 15°C / min, stirred and reacted at a rate of 50r / min for 4h, concentrated under reduced pressure, evaporated to dryness, washed with water, ethyl acetate, methanol and evaporated to dryness, and the washed methanol Liquid drying, obtains 117.3g triacetylganciclovir;

[0040] The N,N-dimethylformamide-methanol solution is obtained by mixing N,N-dimethylformamide and methanol at a volume ratio of 1:2.5;

[0041] The adsorbent is obtained by mixing zeolite molecular sieve and HPD-600 resin in a weight ratio of 1:0.58;

[0042] S2. Ethanol and water are mixed according to the volume ratio of 2:1, then add the sodium hydroxide of ethanol aqueous s...

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Abstract

The invention provides a ganciclovir sodium synthesis process which comprises the following steps: taking diacetylguanine as a raw material, mixing and heating diacetylguanine with p-toluene sulfonic acid and an N, N-dimethylformamide-methanol solution, then adding triacetylmethoxyglycerol for condensation, and adding methanol and an adsorbent in the condensation process so that the reaction is balanced and positively moved, the generation of triacetyl ganciclovir isomers is reduced, the product purity and yield are improved, and finally reaction is performed in a sodium hydroxide ethanol aqueous solution to obtain ganciclovir sodium. The ganciclovir sodium produced by the synthesis process is easy to operate, low in cost and easy to industrially produce.

Description

technical field [0001] The invention relates to the field of medicine, in particular to a synthesis process of ganciclovir sodium. Background technique [0002] Ganciclovir (chemical name 9-(1,3-dihydroxy-2-propoxymethyl)-guanine) is an important member of nucleoside antiviral drugs and is currently one of the best drugs for the treatment of CMV infection. one. However, the impurity of ganciclovir currently prepared is generally above 0.4%, and there is a greater risk in using it for injection. And ganciclovir has the problems of unstable chemical structure and low solubility, and it is prone to dilute-alcohol interconversion phenomenon. When preparing pharmaceutical preparations, especially aqueous solution preparations, a certain amount of co-solvent must be added. If the co-solvent is added too much, then It will inevitably increase the toxic and side effects in clinical use. [0003] Therefore, how to improve its stability and solubility and reduce toxic and side effe...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D473/18
CPCC07D473/18
Inventor 陆一峰蔡亲
Owner HAINAN HAILING CHEMIPHARMA CORP
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