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Preparation method of vidarabine monophosphate

A technology of adenosine vidarabine monophosphate and adenosine vidarabine, which is applied to the preparation of sugar derivatives, chemical instruments and methods, sugar derivatives, etc., which can solve the problems of high cost, easy-to-corrosion equipment, and high equipment requirements, and achieve reduction Response cost, improve production efficiency, and shorten the process route

Inactive Publication Date: 2011-06-01
双鹤药业(海南)有限责任公司
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Problems solved by technology

[0009] The route of the above semi-synthetic method has long reaction steps, and the cyclization at the 8,2'-position requires high temperature and high pressure, and the separation of intermediates is also difficult. H 2 S open loop also needs high pressure and absolute anhydrous, high equipment requirements, easy to corrode equipment, large pollution, easy to cause staff poisoning
After the process improvement of the total synthesis method, benzene and mercury are removed, and the total yield of adenosine vidarabine can reach 32%, but the cost is relatively high, which is not conducive to industrial production

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  • Preparation method of vidarabine monophosphate
  • Preparation method of vidarabine monophosphate
  • Preparation method of vidarabine monophosphate

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Embodiment Construction

[0024] Now the method for synthesizing vidarabine monophosphate of the present invention will be further described in terms of examples:

[0025] According to the preparation method of vidarabine monophosphate of the present embodiment, it comprises the following steps in sequence:

[0026] (1) Take adenosine vidarabine, dissolve it in 1000ml of triethyl phosphate, protect it with nitrogen flow, add 60ml of phosphorus oxychloride dropwise under stirring at low temperature, and keep the reaction at 5°C for 2.5 hours;

[0027] (2) Pour the reaction solution into 1000ml water, keep stirring, add 10g activated carbon for decolorization, add dropwise 40% NaOH solution to adjust PH=8.0, decolorize for 30 minutes, filter with suction, extract the filtrate with 1000ml dichloromethane, and use the organic phase again Wash with water; combine the aqueous phases, add dropwise 40% NaOH to adjust pH=3.0, cool overnight, crystallize, filter, and dry to obtain a crude product.

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Abstract

The invention provides a synthesis process of vidarabine monophosphate, which comprises the steps of: dissolving vidarabine as a raw material in triethyl phosphate, adding phosphorus oxychloride for low-temperature reaction through protection, and carrying out posttreatment, such as decoloring with active carbon and the like, to obtain a crude product of the vidarabine monophosphate. The invention has the advantages of short process route, higher yield and reduced reaction cost. The vidarabine monophosphate is prepared with the method which is simple in operation, thus the industrialized production is easy to realize, and the production efficiency is increased.

Description

technical field [0001] The invention relates to the technical field of synthesis of antiviral drug vidarabine monophosphate. Background technique [0002] Adenosine monophosphate (chemical name: 9-(β-D-arabinofuranosyl) adenine 5'-monophosphate, Ara-AMP), a nucleotide antiviral drug, is adenosine vidarabine (Ara-A) second generation formulation. Its pharmacological effect is to combine with the deoxyribonucleic acid polymerase of the virus to reduce its activity and inhibit DNA synthesis. After adenosine monophosphate enters the cell, it undergoes phosphorylation to generate adenosine diphosphate and adenosine triphosphate. The antiviral activity is mainly caused by vidarabine adenosine triphosphate, which competes with deoxyadenosine triphosphate to bind to viral DNA, thereby selectively inhibiting the activity of viral polymerase and nucleotide reductase, and inhibiting the continuation of viral DNA. synthesis. [0003] Vidarabine monophosphate is a water-soluble deriv...

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07H19/20C07H1/02
Inventor 魏雪纹李强袁芳
Owner 双鹤药业(海南)有限责任公司
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