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Method for preparing 3-N-formylated aminopyrazole compound

A technology for formylating aminopyrazole and aminopyrazole is applied in the field of preparation of 3-N-formylated aminopyrazole compounds, and can solve the difficulty of extracting and purifying 3-N-formylated aminopyrazole compounds, There are no problems such as physical and chemical properties, and even the impact of clinical applications, to achieve the effects of high yield, simple operation and high purity

Inactive Publication Date: 2009-12-16
CHONGQING UNIV
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Problems solved by technology

However, since the content of 3-N-formylated aminopyrazole compounds in allopurinol is extremely small, it has caused great difficulties in extracting and purifying 3-N-formylated aminopyrazole compounds.
So, so far, under the situation that people still can't obtain the 3-N-formylated aminopyrazole compound with higher purity of sufficient quantity, also can't give the 3-N-formylated aminopyrazole compound Effective research on the influence of puranol on physical and chemical properties and even clinical application

Method used

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  • Method for preparing 3-N-formylated aminopyrazole compound
  • Method for preparing 3-N-formylated aminopyrazole compound
  • Method for preparing 3-N-formylated aminopyrazole compound

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Embodiment Construction

[0013] A preparation method of 3-N-formylated aminopyrazole compound, the preparation method comprising the steps of:

[0014] (1) In a reaction vessel, a 3-aminopyrazole compound is dissolved in a mixed solution of an acylating agent and formic acid. Wherein, the volume ratio of the acylating agent to formic acid is 60:1, and according to the concentration of the 3-aminopyrazole compound, the mixed solution of the acylating agent and formic acid is configured in excess to facilitate the complete conversion of the 3-aminopyrazole compound. Then, fully stir under the action of microwave, and heat and keep warm for 40min. Wherein, the microwave power is 900W, and the reaction temperature is 100°C.

[0015] (2) After the reaction is completed, cool to room temperature, and then remove the unreacted acylating agent and formic acid mixed solution by suction filtration to obtain a crude product containing 3-N-formylated aminopyrazole compound.

[0016] (3) Rinse the crude product ...

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Abstract

The invention discloses a method for preparing a 3-N-formylated aminopyrazole compound. The preparation method is a synthetic method for dissolving 3-aminopyrazole compound into mixed solution of acylation agent and formic acid, and adopts microwave-assisted heating technology. The invention discloses the method for directly preparing the 3-N-formylated aminopyrazole compound with simple and convenient operation and high yield and purity so that people can effectively research the influence of the 3-N-formylated aminopyrazole compound on the physicochemical property, even clinical application of allopurinol.

Description

technical field [0001] The present invention relates to a preparation method of 3-N-formylated aminopyrazole compound. Background technique [0002] Allopurinol (allopurinol, allopurinol) is an isomer of hypoxanthine, and its pharmaceutical product is an anti-gout drug—allopurinol and its metabolite oxypurinol can inhibit xanthine oxidase (Xanthine Oxidase) , XO), which prevents the metabolism of hypoxanthine and xanthine into uric acid in the human body, thereby reducing the generation of uric acid. Reduce the uric acid content in blood and urine to a level below the solubility, prevent uric acid from forming crystals and depositing in joints and other tissues, and at the same time, help the redissolution of uric acid crystals in the tissues of gout patients. Due to side reactions occurring in the process of synthesizing allopurinol, 3-N-formylated aminopyrazole compounds with very small content should be derived. Therefore, in the research on the physicochemical properti...

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D231/40B01J31/04
Inventor 刘作华杜军陶长元郑习霞孙大贵左赵宏
Owner CHONGQING UNIV
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