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Pyridino-[1,5-a]pyridine drug and preparation method and composition thereof and application of pyridino-[1,5-a]pyridine drug in nursing of skin ulcer patient

A skin ulcer, 5-a technology, applied in pyrazolo[1,5-a]pyridine drugs and its preparation, application field of skin ulcer patient care, can solve the problem of binding bandages and ulcer wounds

Inactive Publication Date: 2018-12-14
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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  • Pyridino-[1,5-a]pyridine drug and preparation method and composition thereof and application of pyridino-[1,5-a]pyridine drug in nursing of skin ulcer patient
  • Pyridino-[1,5-a]pyridine drug and preparation method and composition thereof and application of pyridino-[1,5-a]pyridine drug in nursing of skin ulcer patient
  • Pyridino-[1,5-a]pyridine drug and preparation method and composition thereof and application of pyridino-[1,5-a]pyridine drug in nursing of skin ulcer patient

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] 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

[0033] 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,...

Embodiment 3

[0035] 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,1...

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Abstract

The invention discloses a pyridino-[1,5-a]pyridine drug and a preparation method and composition thereof and application of the pyridino-[1,5-a]pyridine drug in nursing of a skin ulcer patient, and belongs to the technical field of medicine synthesis. The technical scheme comprises the key points that the pyridino-[1,5-a]pyridine drug molecule has a following molecular structure. The invention also specifically discloses the preparation method of the pyridino-[1,5-a]pyridine drug for skin ulcer care and the application in preparation of the pharmaceutical composition for skin ulcer care. By combining a thiazepine compound which has the advantages of sedation, promotion of growth hormone secretion, anti-ulcer, sterilization and the like, the pyridino-[1,5-a]pyridine drug molecule for skin ulcer care is synthesized, antibacterial activity tests are carried out, and it is showed that the compound had good inhibitory activity against Staphylococcus epidermidis and Staphylococcus aureus which easily give rise to skin ulcer.

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, its preparation method, composition and its application in the care of patients with skin ulcers. 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...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D519/00A61K31/519A61P17/02A61P31/04
CPCA61P17/02A61P31/04C07D519/00
Inventor 李小莉庞琳薇田子巧陈昊李启华习红利李莉莉
Owner THE FIRST AFFILIATED HOSPITAL OF HENAN UNIV OF SCI & TECH
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