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Doxofylline impurity and preparation method thereof

A compound and reaction technology, applied in the field of chemical analysis, can solve the problems of rapid onset of action and long duration of drug effect, and achieve the effects of improving quality, improving accurate positioning and qualitative, and strengthening control

Active Publication Date: 2019-05-10
四川蓝励医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

In addition, the bronchial smooth muscle relaxation effect of doxofylline is more than 10 times that of aminophylline, and the onset of effect is fast and the drug effect time is long.

Method used

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  • Doxofylline impurity and preparation method thereof
  • Doxofylline impurity and preparation method thereof
  • Doxofylline impurity and preparation method thereof

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Embodiment Construction

[0031] It should be understood that the specific embodiments described here are only used to explain the present invention, not to limit the present invention.

[0032] The embodiment of the present invention proposes a compound with the structure shown in Formula 1:

[0033]

[0034] The embodiment of the present invention also provides a compound of formula 1 (ie 9-(2,2-dimethoxyethyl)-1,3-dimethyl-1H-purine-2,6(3H,9H)-dione ) synthesis path, as follows:

[0035]

[0036]

[0037] In one embodiment, the reaction to generate the compound of formula 1-2 (i.e. 6-chloro-1,3-dimethylpyrimidine-2,4(1H,3H)-dione (1-2)) is as follows:

[0038]

[0039] In this embodiment, the reaction steps of implementation are specifically as follows:

[0040] 1) The compound of formula 1-1 (20.0g) was dissolved in phosphorus oxychloride (155mL), lowered to 0°C, and water (6.45mL) was slowly added dropwise. After the dropwise addition, it was slowly raised to room temperature and rea...

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Abstract

The invention provides a doxofylline impurity and a preparation method thereof. The impurity is 9-(2,2-dimethoxyethyl)-1,3-dimethyl-1H-purine-2,6(3H,9H)-diketone. A compound provided by the inventioncan be used as a standard substance for detecting ingredients of a doxofylline finished product, thereby improving the accurate positioning and characterization of the detection and analysis of doxofylline finished product for the impurities, strengthening the control of the impurities, and further improving the quality of the doxofylline finished products.

Description

technical field [0001] The invention relates to the field of chemical analysis, in particular to a doxofylline impurity and a preparation method thereof. Background technique [0002] Doxofylline (Doxofylline), the chemical name is 1,3-dimethyl-7-(1,3-dioxol-2-yl)methyl-3,7-dihydro-1H-purine- 2,6-diketones. Doxofylline is a bronchodilator drug that was launched in Italy in 1988 under the name Anismar. The safety of doxofylline is higher than that of theophylline, and it is a new generation of methylpurine derivatives that can replace theophylline drugs. Doxofylline is clinically used in the treatment of bronchial asthma, chronic obstructive pulmonary disease and other diseases such as dyspnea caused by bronchospasm. Its mechanism of action is to control the chronic inflammation of the respiratory tract by inhibiting the release of various inflammatory mediators and cytokines development of. Inhibit phosphodiesterase activation of proteases A and G in airway smooth muscle...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D473/08
Inventor 王昌贵胡观明熊涛陈晓晖
Owner 四川蓝励医药科技有限公司
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