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Pyrazolo [1,5-a]pyridine pharmaceutical molecules used for skin ulcer nursing and preparation method and application thereof

A technology for skin ulcers and drug molecules, which can be used in skin diseases, drug combinations, pharmaceutical formulations, etc., and can solve the problems of binding bandages and ulcer wounds.

Inactive Publication Date: 2018-07-27
THE FIRST AFFILIATED HOSPITAL OF HENAN UNIV OF SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

After bandaging the patient's skin ulcer, if the ulcer is not relieved well, it will cause the bandage to adhere to the ulcer wound. During the dressing change process, changing the bandage will cause great pain to the patient. Therefore, how to treat the patient's skin ulcer Effective care has always been a matter of great concern to medical staff

Method used

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  • Pyrazolo [1,5-a]pyridine pharmaceutical molecules used for skin ulcer nursing and preparation method and application thereof
  • Pyrazolo [1,5-a]pyridine pharmaceutical molecules used for skin ulcer nursing and preparation method and application thereof
  • Pyrazolo [1,5-a]pyridine pharmaceutical molecules used for skin ulcer nursing and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Under nitrogen protection, the compound Add 15g (0.1mol) into 150mL of 1,4-dioxane, then add 30g of deionized water, 15g (0.12mol) of 2-thiophene boronic acid and 32g (0.15mol) of potassium phosphate, replace the nitrogen in the reaction system Gas three times, then add the catalyst Pd(dppf)Cl 2 0.3g, continue to replace the gas in the reaction system with nitrogen for three times and heat to 90°C for reaction. After 3 hours of reaction, LCMS monitors the complete reaction of raw materials, cool to room temperature, add 200mL of ethyl acetate to extract the reaction solution three times, combine the organic phases, and use saturated chlorine The organic phase was washed once with 200 mL of sodium chloride solution, dried with anhydrous magnesium sulfate, concentrated and purified by column chromatography (V methanol:V dichloromethane=2:1) ​​to obtain the compound 16g, the yield is 80%; 1 H NMR (CDCl 3 ,400MHz)δ8.91(d,J=8.0Hz,1H),8.37(d,J=8.0Hz,1H),7.77-7.75(m,2H),...

Embodiment 2

[0030] Under nitrogen protection, the compound Add 15g (0.1mol) to 150mL of 1,4-dioxane, then add 30g of deionized water, 15g (0.12mol) of 2-thiophene boronic acid and 20.7g (0.15mol) of potassium carbonate, and replace the reaction system with nitrogen gas three times, then add the catalyst Pd(dppf)Cl 2 0.3g, continue to replace the gas in the reaction system with nitrogen for three times and then heat to 90°C for reaction. After 3 hours of reaction, LCMS monitors the complete reaction of raw materials, cools to room temperature, adds 200mL of ethyl acetate to extract the reaction solution three times, combines the organic phases, and The organic phase was washed once with 200 mL of sodium chloride solution, dried with anhydrous magnesium sulfate, concentrated and purified by column chromatography (V methanol:V dichloromethane=2:1) ​​to obtain the compound 15g, the yield is 75%; 1 H NMR (CDCl 3 ,400MHz)δ8.91(d,J=8.0Hz,1H),8.37(d,J=8.0Hz,1H),7.77-7.75(m,2H),7.62-7.61(m,1...

Embodiment 3

[0032] Under nitrogen protection, the compound Add 15g (0.1mol) to 150mL of 1,4-dioxane, then add 30g of deionized water, 15g (0.12mol) of 2-thiophene boronic acid and 15g (0.15mol) of potassium bicarbonate, and replace the reaction system with nitrogen gas three times, then add the catalyst Pd(dppf)Cl 2 0.3g, continue to replace the gas in the reaction system with nitrogen for three times and then heat to 90°C for reaction. After 3 hours of reaction, LCMS monitors the complete reaction of raw materials, cools to room temperature, adds 200mL of ethyl acetate to extract the reaction solution three times, combines the organic phases, and The organic phase was washed once with 200 mL of sodium chloride solution, dried with anhydrous magnesium sulfate, concentrated and purified by column chromatography (V methanol:V dichloromethane=2:1) ​​to obtain the compound 9g, the yield is 45%; 1 H NMR (CDCl 3 ,400MHz)δ8.91(d,J=8.0Hz,1H),8.37(d,J=8.0Hz,1H),7.77-7.75(m,2H),7.62-7.61(m,1H...

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Abstract

The invention discloses pyrazolo [1,5-a]pyridine pharmaceutical molecules used for skin ulcer nursing and a preparation method and an application thereof, which belong to the technical field of medicine synthesis. The technical scheme has the main points that the pyrazolo [1,5-a]pyridine pharmaceutical molecules have a following molecular structure shown as the specification. The invention also discloses the preparation method of the pyrazolo [1,5-a]pyridine pharmaceutical molecules and the application of the pyrazolo [1,5-a]pyridine pharmaceutical molecules in preparation of a pharmaceuticalcomposition for skin ulcer nursing. The thiazepin compounds have the advantages of keeping calm, promoting growth hormone secretion, resisting ulcer, and sterilizing; the pyrazolo [1,5-a]pyridine pharmaceutical molecules can be synthesized and an antibacterial activity test is carried, the compound has good inhibition activity on bacillus anthracis and staphylococcus due to skin ulcer, a drug ointment is prepared, a clinical nursing experiment is carried out, and the nursing effect is obvious.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical synthesis, and in particular relates to a pyrazolo[1,5-a]pyridine drug molecule used for skin ulcer care and its preparation method and application. Background technique [0002] Skin ulcer is a common secondary damage to the skin. The skin defect or damage reaches the dermis or below the dermis. It is single or multiple. The ulcer expands rapidly in the acute stage, and the surface is covered with necrotic tissue, exudate, and scab. The skin around the ulcer is red and swollen. The etiology is complicated, the course of the disease is long, and it is easy to repeat. After bandaging the patient's skin ulcer, if the ulcer is not relieved well, it will cause the bandage to adhere to the ulcer wound. During the dressing change process, changing the bandage will cause great pain to the patient. Therefore, how to treat the patient's skin ulcer Effective care has always been a matter of great co...

Claims

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Application Information

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IPC IPC(8): C07D519/00A61K31/519A61K9/06A61P17/02A61P31/04A61P31/02
CPCA61P17/02A61P31/04C07D519/00
Inventor 李小莉庞琳薇田子巧习红丽李莉莉
Owner THE FIRST AFFILIATED HOSPITAL OF HENAN UNIV OF SCI & TECH
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