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Nitrogen heterocyclic compound preparation method and application thereof

A technology of compound and nitrogen heterocycle, which is applied in the field of preparation of nitrogen heterocycle compounds, can solve problems such as the synthetic preparation method and separation and purification method of green-like substances that have not been seen

Active Publication Date: 2013-04-24
北京华禧联合科技发展有限公司
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Problems solved by technology

Based on the above reasons, in the research process of developing azedipine pharmaceutical preparations, it is necessary to strictly control the content of green substances in raw materials and pharmaceutical preparations. Related reports

Method used

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  • Nitrogen heterocyclic compound preparation method and application thereof
  • Nitrogen heterocyclic compound preparation method and application thereof
  • Nitrogen heterocyclic compound preparation method and application thereof

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preparation example Construction

[0024] In a typical embodiment of the present invention, the preparation method of the nitrogen-heterocyclic compound having the structural formula I includes the following steps: A. Oxidation reaction of the azendipine bulk drug with an oxidizing agent to obtain a mixture; B. Isolating the compound having the structural formula I nitrogen heterocyclic compounds. In the above preparation method, the azedipine bulk drug is mixed with an oxidizing agent to undergo an oxidation reaction, so that the azedipine bulk drug is completely converted into a nitrogen-heterocyclic compound with the structural formula I, and then the nitrogen-heterocyclic compound with the structural formula I The compound is separated and purified from the reaction mixture to obtain a relatively high-purity nitrogen heterocyclic compound with structural formula I, which is used as a standard product in the control experiment and used for the research on the quality control of the azedipine pharmaceutical pr...

Embodiment 1

[0037] In 10ml of dichloromethane, add 1g of azendipine crude drug to dissolve it, add 10ml of hydrogen peroxide, stir and react at 30°C for 60 minutes; add 20ml of dichloromethane, let stand to separate the layers, and separate the organic phase; Concentrate under pressure until there is no volatile matter to obtain a concentrate; add 10ml of methanol to the concentrate to dissolve it, cool to 0-5°C and stir for 2 hours, a solid precipitates, filter, wash the filter cake with a small amount of methanol, and dry under reduced pressure at 40°C , to obtain nitrogen heterocyclic compounds with the structural formula I.

[0038] The yield of the obtained nitrogen heterocyclic compound with structural formula I was 89.0%; the purity of the nitrogen heterocyclic compound with structural formula I detected by high resolution liquid chromatography (HPLC) was 97.4%.

Embodiment 2

[0040] In 50ml of dichloromethane, add 5g of azendipine bulk drug to dissolve it, add 100ml of hydrogen peroxide, stir and react at 30°C for 65 minutes; Concentrate under pressure until there is no volatile matter to obtain a concentrate; add 50ml of methanol to the concentrate to dissolve it, cool down to 0-5°C and stir for 4 hours, a solid precipitates, filter, wash the filter cake with a small amount of methanol, and dry under reduced pressure at 40°C , to obtain nitrogen heterocyclic compounds with the structural formula I.

[0041] The yield of the obtained nitrogen heterocyclic compound with structural formula I was 87.8%; the purity of the obtained nitrogen heterocyclic compound with structural formula I detected by high resolution liquid chromatography (HPLC) was 98.5%.

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Abstract

The invention provides a nitrogen heterocyclic compound preparation method and application thereof. The nitrogen heterocyclic compound preparation method includes that A azelnidipine bulk drugs have an oxidizing reaction with oxidizing agent and compound is achieved, B. nitrogen heterocyclic compound with a structural formula I is separated from the compound, through the nitrogen heterocyclic compound preparation method, the azelnidipine bulk drugs and the oxidizing agent are mixed and have the oxidizing reaction, so that the azelnidipine bulk drugs are completely converted into the nitrogen heterocyclic compound with the structural formula I, then the nitrogen heterocyclic compound with the structural formula I is separated and purified from reaction compound, and the achieved nitrogen heterocyclic compound with the structural formula I is high in purity, served as standard substance in a control experiment, and used for studying quality control of azelnidipine medicinal preparations.

Description

technical field [0001] The invention relates to the field of chemical synthesis, in particular to a preparation method and application of nitrogen heterocyclic compounds. Background technique [0002] Azedipine belongs to dihydropyridine calcium channel blockers (CCB). Calcium channel blockers are widely used as first-line hypertension treatment drugs due to their reliability in reducing blood pressure. [0003] Azedipine was developed with the goal of "an ideal CCB antihypertensive drug with mild and long-lasting antihypertensive effect and less stimulation to the heart". The antihypertensive effect of this drug is very similar to that of the third-generation dihydropyridine CCB drug amlodipine, and the effect lasts for a long time and the effect is mild. However, azedipine differs from amlodipine in pharmacological properties such as effects on the heart and affinity for blood vessels, and is less likely to cause excitation of the sympathetic nervous system such as tachyc...

Claims

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Application Information

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IPC IPC(8): C07D401/12G01N33/15
Inventor 毕华谢晓东
Owner 北京华禧联合科技发展有限公司
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