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Synthetic method doxazosin impurity

A doxazosin and synthesis method technology, applied in the field of medicine, can solve the problems of poor qualitative and quantitative accuracy and high risk, and achieve the effects of low synthesis cost, short reaction route and low energy consumption

Active Publication Date: 2018-07-13
HEFEI HUAFANG PHARMA SCI & TECH
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] The European Pharmacopoeia and the United States Pharmacopoeia doxazosin mesylate standards do not record this impurity Ⅰ, and there is no report on the synthesis method of this impurity in domestic and foreign literatures and patents, and there is no impurity Ⅰ in the synthesis process of doxazosin mesylate at home and abroad For the supply of reference substances, the self-control method is currently used, but its qualitative and quantitative accuracy is not good, and the risk of clinical drug use is high

Method used

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  • Synthetic method doxazosin impurity
  • Synthetic method doxazosin impurity
  • Synthetic method doxazosin impurity

Examples

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Effect test

Embodiment 1

[0024] A method for synthesizing doxazosin impurities, comprising the steps of: mixing 5ml of n-butanol, 0.24g of 2-chloro-4-hydroxyl-6,7-dimethoxyquinazoline, 0.28g of N-(1, 4-Benzodioxane-2-carbonyl)piperazine was added into the three-necked flask, heated to reflux, stirred for 1 h, cooled, filtered and dried at 50°C to obtain 0.42 g of doxazosin impurity with a yield of 95 %, wherein, the reaction equation of the above-mentioned doxazosin impurity preparation is as follows:

[0025]

Embodiment 2

[0027] A method for synthesizing doxazosin impurities, comprising the steps of: mixing 50ml of ethanol, 2.2g of 2-chloro-4-hydroxy-6,7-dimethoxyquinazoline, 2.8g of N-(1,4- Benzodioxane-2-carbonyl)piperazine was added to the three-necked flask, heated to 80°C, and stirred for 5 hours under reflux. After cooling, filtration and drying at 40°C, 3.73 g of doxazosin impurity was obtained with a yield of 90 %, wherein, the reaction equation of the above-mentioned doxazosin impurity preparation is as follows:

[0028]

Embodiment 3

[0030] A method for synthesizing doxazosin impurities, comprising the steps of: mixing 50ml of methanol, 2.4g of 2-chloro-4-hydroxy-6,7-dimethoxyquinazoline, 2.6g of N-(1,4- Benzodioxane-2-carbonyl)piperazine was added to the three-necked flask, heated to 70°C, stirred for 8 hours, cooled, filtered and dried at 60°C to obtain 3.57g of doxazosin impurities, with a yield of 85% , wherein, the reaction equation of the above-mentioned doxazosin impurity preparation is as follows:

[0031]

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Abstract

The invention discloses a synthetic method a doxazosin impurity. The synthetic method comprises following steps: a solvent, 2-chloro-4-hydroxy-6,7-dimethoxyquinazoline, and 1-(1,4-Benzodioxane-2-carbonyl)piperazine are introduced into a reaction, heating stirring is carried out for complete reaction, and cooling, filtering, and drying are carried out so as to obtain the doxazosin impurity. The synthetic method is capable of obtaining the high purity doxazosin impurity, the doxazosin impurity can be taken as a reference substance, the reaction route is short, the yield is high, the energy consumption is low, the synthesis cost is low, operation is simple, and the synthetic method is suitable for large scale preparation.

Description

technical field [0001] The invention relates to the technical field of medicines, in particular to a method for synthesizing doxazosin impurities. Background technique [0002] Hypertension is one of the leading causes of death globally, with approximately 7.7 million deaths globally attributable to hypertension in 2010. In China, 50% of patients with cardiovascular chronic kidney disease and diabetes die from high blood pressure. The awareness rate, control rate, and treatment rate of hypertension have improved significantly in recent decades, which is due to my country's great efforts, but the prevalence of hypertension is still 28%, showing an increasing trend. In 2016, a sub-journal of "JAMA" published a cohort study on hypertension in my country, revealing the burden and basic situation of hypertension in China, revealing that the burden of hypertension in my country is shocking: among the 500,233 residents who participated in the survey, the prevalence of hypertension...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D405/12
CPCC07D405/12
Inventor 高永好何勇吴宗好
Owner HEFEI HUAFANG PHARMA SCI & TECH
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