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Diazoxide preparation method

A technology of diazoxide and compounds, applied in the field of preparation of diazoxide, can solve problems such as unfavorable industrial production, harsh reaction temperature, long reaction route, etc., and achieves less stringent reaction temperature requirements, mild process reaction conditions, and solvent toxicity. small effect

Pending Publication Date: 2018-07-10
XUZHOU WANBANG JINQIAO PHARMA +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] There are few references on the synthesis route and preparation method of diazoxide, and the route sorted out according to the prior art is as follows. The disadvantage is that the reaction route is long, the solvent toxicity is large, and the reaction temperature is harsh; it is not conducive to industrial production

Method used

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Examples

Experimental program
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Effect test

Embodiment 1

[0032] Preparation of compound 3:

[0033]

[0034] Add p-compound 1 (100g) and chlorobenzene (560ml) into a 1L flask, stir and heat to dissolve, set aside. Add compound 2 (120g) and chlorobenzene (280ml) into a 2L three-necked flask, stir and cool down to 10°C, add the spare p-chloroaniline solution dropwise, and control the temperature during the dropping process at 10°C. Add aluminum trichloride (100g) after dropping, remove the cooling bath, then slowly heat up to 100°C to react for 2 hours, stop heating, and lower the temperature. Prepare another 3L three-necked bottle, add water (1L), and under rapid stirring, slowly pour the reaction solution into water, stir, and suction filter. The filter cake was air-dried for 5 hours to obtain compound 3 with a yield of 59.6% and a purity of 97.7%.

[0035] Preparation of diazoxide:

[0036]

[0037] Add compound 3 (100g), acetic acid (500g) and 98% sulfuric acid (350g) into a 2L three-necked flask and stir, slowly heat to ...

Embodiment 2

[0039] Preparation of compound 3:

[0040]

[0041] Add p-compound 1 (100g) and chlorobenzene (560ml) into a 1L flask, stir and heat to dissolve, set aside. Add compound 2 (120g) and chlorobenzene (280ml) into a 2L three-necked flask, stir and cool down to 10°C, add the spare p-chloroaniline solution dropwise, and control the temperature during the dropping process at -10°C. Add aluminum trichloride (100g) after dropping, remove the cooling bath, then slowly heat up to 100°C to react for 2 hours, stop heating, and lower the temperature. Prepare another 3L three-necked bottle, add water (1L), and under rapid stirring, slowly pour the reaction solution into water, stir, and suction filter. The filter cake was air-dried for 5 hours to obtain compound 3 with a yield of 59.8% and a purity of 98.5%.

[0042] Preparation of diazoxide:

[0043]

[0044] Add compound 3 (100g), acetic acid (500g) and 98% sulfuric acid (350g) into a 2L three-necked flask and stir, slowly heat to 1...

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Abstract

The invention discloses a diazoxide preparation method which includes the steps of (1), subjecting a compound 1 and a compound 2 to low-temperature reaction in a solvent 1, carrying out high-temperature reaction 1 under action of a catalyst to obtain a compound 3; (2), adding a good amount of acetic acid and a solvent 2 in the compound 3, and carrying out high-temperature reaction 2 to obtain diazoxide. The diazoxide preparation method is simple, convenient, economic and environmental friendly; raw materials for preparing diazoxide by the method are easy to obtain; besides, preparation processis simple, reaction conditions are mild, requirements on equipment conditions are not high, reaction time is short, yield is increased, by-products are reduced, post-treatment is easy to carry out,and the preparation method is adaptable to large-scale industrial production and has good industrialization prospect.

Description

technical field [0001] The invention belongs to the technical fields of organic synthesis route design and medicine and chemical industry, and specifically relates to a synthesis method of a compound used for relaxing vascular smooth muscle, reducing peripheral vascular resistance and inhibiting pancreatic beta cells from secreting insulin, and more specifically relates to a A preparation method of diazoxide. Background technique [0002] Diazoxide can relax vascular smooth muscle, reduce peripheral vascular resistance, and cause a sharp drop in blood pressure. A rapid intravenous injection of 300 mg of this product can produce a peak antihypertensive within 5 minutes, reducing blood pressure to a normal level and maintaining it for 2 to 18 hours or longer. While lowering the blood pressure, it does not reduce the cardiac output, so the blood flow of the brain, kidneys, and coronary arteries remains unchanged. It is suitable for first aid in hypertensive crisis. Diazoxide...

Claims

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Application Information

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IPC IPC(8): C07D285/24
CPCC07D285/24
Inventor 王飞林彬乔德水
Owner XUZHOU WANBANG JINQIAO PHARMA
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