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Preparation method of vidarabine monophosphate

A technology of adenosine vidarabine monophosphate and adenosine vidarabine, which is applied in the field of preparation of adenosine vidarabine monophosphate, which can solve the problems of large environmental pollution and achieve the effects of small environmental pollution, easy separation and purification, and low cost

Active Publication Date: 2015-11-11
海南卓科制药有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] In view of this, the present invention provides a method for preparing vidarabine monophosphate, which solves the technical problem of relatively large environmental pollution in the process of preparing vidarabine monophosphate in the prior art

Method used

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  • Preparation method of vidarabine monophosphate

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Embodiment 1

[0023] A preparation method of vidarabine monophosphate, comprising the following steps:

[0024] 1) Prepare the reaction solution: Add 700ml deionized water, 1.1mol glycerin, 0.4ml TritonX-100, 0.007mol magnesium sulfate and 0.1mol ATP.Na to a 2L Erlenmeyer flask 2 , and then adjust the pH value of the solution to 7.5±0.1 with 10NNaOH (about 15ml~20ml) under stirring; add 124mg dithiothreitol to the above solution and stir to dissolve, add deionized water to a total volume of 800ml; add 0.1molAra -A, after stirring evenly, heat in a water bath until the internal temperature reaches 27°C±2°C.

[0025] 2) Enzymatic synthesis reaction: Add creatine kinase to the solution to make the concentration 1.0×10 -3 mmol / L, heat in a water bath at 27°C±2°C and start the timing reaction; during the reaction period, the pH value of the solution needs to be detected in time, when the pH value reaches 7.2±0.3, slowly add ammonia water to the solution to restore the pH value to 7.5±0.1; Afte...

Embodiment 2

[0028] A preparation method of vidarabine monophosphate, comprising the following steps:

[0029] 1) Prepare the reaction solution: add 700L deionized water, 1100mol glycerin, 0.4L TritonX-100, 9.03mol magnesium chloride and 100molATP.Na to a 2000L reactor 2 ; Then use 10NNaOH (about 15-20L) to adjust the pH value of the solution to 9.0±0.1 under stirring; add 124g dithiothreitol and 100mol Ara-A in batches to the solution, stir at a speed of 60Hz during the addition, and test again after stirring evenly The pH value can be adjusted to 9.0±0.1 with ammonia water, and the reaction temperature is controlled to be 32°C±2°C.

[0030] 2) Enzymatic synthesis reaction: reduce the stirring speed to 35Hz, add creatine kinase to the above solution to make the concentration 1.0×10 -5 mmol / L, heat the reaction kettle at 32°C±2°C in a closed state and start the timing reaction; during the reaction, check the pH value of the solution in time, and when the pH value reaches 7.2±0.3, slowly a...

Embodiment 3

[0034] A preparation method of vidarabine monophosphate, comprising the steps of:

[0035] 1) Prepare the reaction solution: Add 700ml deionized water, 1.5mol glycerin, 0.4ml TritonX-100, 0.02mol magnesium acetate tetrahydrate and 0.1mol ATP.Na to a 2L Erlenmeyer flask 2 , then adjust the pH value of the solution to 8.3±0.1 with 10NNaOH (about 15ml~20ml) under stirring; add 124mg dithiothreitol to the above solution and stir to dissolve, add deionized water to a total volume of 800ml; add 0.4mol Ara-A, stirred evenly, heated in a water bath until the internal temperature reached 43°C±2°C.

[0036] 2) Enzymatic synthesis reaction: Add phosphokinase to the solution to make the concentration 1.0×10 -3 mmol / L, heat in a water bath at 43°C±2°C and start the timing reaction; during the reaction period, the pH value of the solution needs to be detected in time, when the pH value reaches 7.2±0.3, slowly add ammonia water to the solution to restore the pH value to 8.3±0.1 ; After 24 ...

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Abstract

The invention discloses a preparation method of vidarabine monophosphate. According to the preparation method, vidarabine monophosphate is obtained by carrying out enzymatic synthesis reaction through adding reaction enzyme into beta-D-vidarabine serving as a starting material, and filtering and devitrifying. The preparation method specifically comprises the following steps: (1) preparing a reaction liquor: stirring deionized water, ATP.Na2, beta-D-vidarabine, glycerol and magnesium ion solution to obtain a mixed solution, adding an alkaline solution into the mixed solution, adjusting the pH to be 7.5-9.0, and adding dithiothreitol, and thus preparing the reaction liquor; (2) carrying out enzymatic synthesis reaction: adding reaction enzyme into the reaction liquor for enzymatic synthesis reaction, wherein the pH of the reaction liquor is 7.6-8.6, and the reaction time is 24h-72h; and (3) filtering and devitrifying: cooling the reaction liquor after enzymatic synthesis reaction in the step (2), filtering to obtain a filtrate, cooling the filtrate for devitrification, and filtering again, and thus obtaining vidarabine monophosphate. The preparation method is low in cost, the product is easy to separate and purify, and high in purity, and the pollution to the environment is small.

Description

technical field [0001] The invention relates to the technical field of preparation of antiviral drugs, in particular to a preparation method of adenosine vidarabine monophosphate. Background technique [0002] Vidarabinemonophosphate (Am-AMP) is the monophosphate compound of β-D-arabinosine (Ara-A), and it is a synthetic adenosine antiviral drug. At present, it is mainly used for chronic viral hepatitis, herpes simplex virus, herpes zoster virus, vaccinia virus, various animal herpes viruses and a few carcinogenic RNA viruses in China. Vidarabine monophosphate has been listed in Europe, the United States, Japan and many other countries. Since the clinical dosage of adenosine vidarabine monophosphate is very large, in order to meet the needs of clinical medication, it is very necessary to develop a synthetic process for adenosine monophosphate which is suitable for industrial production. The existing preparation methods of vidarabine monophosphate mainly include chemical me...

Claims

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Application Information

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IPC IPC(8): C12P19/32
Inventor 魏雪纹
Owner 海南卓科制药有限公司
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