Novel method for synthesizing adenine

A new type of adenine technology, applied in the field of adenine preparation, can solve the problems of many side reactions, increased input costs, cumbersome post-processing, etc., and achieve the effect of reducing production costs and increasing the total yield

Inactive Publication Date: 2018-01-19
SUQIAN YUANYANG BIOTECH
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Problems solved by technology

[0002] Adenine, the chemical name is 6-aminopurine, and the chemical formula is C5H5N5. It is a component of nucleic acid and participates in the synthesis of genetic material; it is an intermediate of many pharmaceutical raw materials, mainly used in the production of vitamin B4 and plant hormone 6-benzyl adenine , adenosine and other pharmaceutical raw materials; its phosphate can promote the proliferation of leuk

Method used

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Example Embodiment

[0014] The examples described in the present invention are illustrative of the present invention and cannot be used to limit the present invention. Any changes and adjustments within the meaning and scope equivalent to the present invention should be considered to be within the scope of the present invention.

[0015] A new method of synthesizing adenine includes the following steps:

[0016] (1) First disperse acetylhypoxanthine in 1,2-dichloroethane, then add it to the reaction kettle, slowly add anhydrous pyridine and triethylamine, stir and heat to 110℃-120℃, add trichlorooxy Phosphorus heat preservation reaction for 50-80 minutes, continue the heat preservation reaction at 110°C-120°C for 4-6 hours, then lower the temperature to about 15°C, and let it stand overnight;

[0017] (2) Filter the above reaction solution and add it to the ammonia / methanol mixture to perform ammonolysis and dry to obtain crude adenine;

[0018] (3) Put the obtained crude adenine into the reactor, after ...

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Abstract

The invention discloses a novel method for synthesizing adenine. The novel method comprises the following steps: (1) firstly, dispersing acetyl hypoxanthine into 1,2-dichloroethane; then adding the mixture into a reaction kettle; slowly adding anhydrous pyridine and triethylamine; stirring and raising the temperature to 110 DEG C to 120 DEG C; adding phosphoryl chloride and keeping heat and reacting for 50min to 80min; continually keeping the heat and reacting at 110 DEG C to 120 DEG C for 4h to 6h; then cooling to about 15 DEG C and standing; (2) filtering a reaction solution; then adding a mixed solution and carrying out aminolysis; drying to obtain an adenine crude product; (3) adding the obtained adenine crude product into the reaction kettle; after finishing feeding, raising the temperature to 80 DEG C and dissolving; after completely dissolving the adenine, adding active carbon and de-coloring; continually keeping the heat at 80 DEG C and de-coloring for 2h; filtering and separating the active carbon; (4) after filtering, carrying out the aminolysis, crystallization and drying to obtain an adenine pure product. The novel method disclosed by the invention takes the acetyl hypoxanthine as a raw material, and the raw material is a byproduct of a glutamic acid fermentation process and is cheap and easy to obtain; the total yield is improved.

Description

technical field [0001] The invention relates to the technical field of preparation of adenine, in particular to a novel method for synthesizing adenine. Background technique [0002] Adenine, the chemical name is 6-aminopurine, and the chemical formula is C5H5N5. It is a component of nucleic acid and participates in the synthesis of genetic material; it is an intermediate of many pharmaceutical raw materials, mainly used in the production of vitamin B4 and plant hormone 6-benzyl adenine , adenosine and other pharmaceutical raw materials; its phosphate can promote the proliferation of leukocytes and increase the number of leukocytes, and is used to prevent and treat leukopenia caused by various reasons, especially for leukopenia caused by tumor chemotherapy. It is used for acute granulocytopenia, but there are many reaction steps for synthesizing adenine, many side reactions, and the post-treatment is very cumbersome, it is difficult to obtain pure products, and the input cos...

Claims

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Application Information

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IPC IPC(8): C07D473/34
Inventor 袁雪生
Owner SUQIAN YUANYANG BIOTECH
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