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Alkyl pyrazine phenolsulfonate and its preparation method and use

A technology of calcium hydroxybenzenesulfonate and medicines, which is applied in the direction of pharmaceutical formulas, active ingredients of anhydride/acid/halide, medical preparations containing active ingredients, etc., and can solve problems such as unsatisfactory curative effect, unbearable pain, and high cost

Inactive Publication Date: 2006-10-11
于学敏
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Laser coagulation treatment has a great relationship with equipment and technology. The treatment is mainly concentrated in big cities and large hospitals. The number of treatments (8-10 times) is high, the cost is high, and the treatment process is painful.
Other microvascular and macrovascular lesions of the heart, brain, kidney, and lung caused by diabetes, hypertension, ischemia, hypoxia, hyperlipidemia, and high blood viscosity have a high incidence rate, and the curative effect of existing drugs is not ideal.

Method used

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  • Alkyl pyrazine phenolsulfonate and its preparation method and use
  • Alkyl pyrazine phenolsulfonate and its preparation method and use
  • Alkyl pyrazine phenolsulfonate and its preparation method and use

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037] Weigh 20.9g of calcium dobesilate, add 60ml of water and stir to dissolve, add another 17.2g of ligustrazine hydrochloride, add 50ml of water and stir to dissolve, heat the two liquids to 80°C respectively, mix and react for 1h under stirring, and cool the reaction solution to 0°C , filtered and dried.

[0038] Product Properties: It is soluble in acidic aqueous solution, slightly soluble in water, slightly soluble in methanol and acetone, very slightly soluble in ethanol, insoluble in ether. Its aqueous solution is acidic, with a pH of 2-4. m·p· ranges from 218°C to 220°C. Appearance is light yellow crystal or crystalline powder, and becomes white powder after dehydration.

[0039] Take about 10mg of this product, add 5ml of water to dissolve, add 2 drops of dilute nitric acid, stir well, add 2 drops of potassium iodide test solution, and an orange-red solution is formed.

[0040] Take this product and add water to make a solution with a water content of about 15 μg...

Embodiment 2

[0050] Weigh 12.9g of hydroquinone, add 11.7ml of concentrated sulfuric acid (93% content ratio) and heat up to 95°C under stirring, keep the temperature down to 80°C for 2 hours, add 40ml of 80°C hot water to dissolve, and heat filter. Separately weigh 13.6g of ligustrazine, add 40ml of ethanol, back distill for 1h, mix the two solutions, heat and stir for 1h, cool to 0°C, filter with suction, recrystallize, and dry. Confirmed by the structure, the product is the same as in Example 1.

Embodiment 3

[0052] Weigh 20.9 g of calcium dobesilate, add 60 ml of water, stir to dissolve, and heat to 80°C. Weigh 13.6g of ligustrazine, add 50ml of ethanol and reflux for 1h. The two liquids were mixed and stirred for 1 hour, cooled to crystallize, recrystallized and dried. Confirmed by the structure, the product is the same as in Example 1.

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PUM

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Abstract

The invention relates to alkyl pyrazine dobesilate monohydrate compounds or their hydrates having formula (I), wherein R is C1-C5 alkyl, a is an integer of 1-5, b is an integer of 1-4, m and n are identical or different, the preparing process is also disclosed. The medicament can be used for the preventing and treating blood capillary pathology of diabetic retina, kidney, peripheral nerve and skin pruritus, and for preventing and treating angina pectoris, myocardial infarction, cerebral embolism, lacuna brain infarction, brain thrombogenesis and brain blood supply insufficiency.

Description

technical field [0001] The present invention relates to an alkylpyrazine dobesilate compound or a mixture thereof and a preparation method thereof. The compound or mixture and a preparation thereof are used for preventing and treating microvascular diseases such as diabetic retina, kidney, peripheral nerve, skin itching, and Angina pectoris, myocardial infarction, cerebral embolism, lacunar infarction, cerebral thrombosis, insufficient blood supply to the heart and brain caused by diabetes, hypertension, ischemia and hypoxia, hyperlipidemia or hyperviscosity. It belongs to the field of medicine. Background technique [0002] Diabetes, hypertension, etc. can be complicated by a variety of clinically difficult diseases, such as fundus disease, kidney, cardiovascular and cerebrovascular, peripheral nerve and other microvascular and macrovascular diseases. Especially the retinopathy (diabetic reticulopathy) that diabetes causes, the medicine that is used for clinical mainly is ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D241/12A61K9/02A61K9/06A61K9/14A61K9/20A61K9/48A61K31/185A61K31/4965C07C309/42
Inventor 于学敏
Owner 于学敏
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