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Composition and application thereof in drug for resisting acute gout

A kind of acute gout, composition technology, applied in the field of organic synthesis and medicinal chemistry, can solve aplastic anemia, neutropenia and other problems

Inactive Publication Date: 2016-02-24
NANJING GUANGKANGXIE BIOLOGICAL MEDICAL TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although they have fast anti-inflammatory and analgesic effects, their toxic and side effects are also quite obvious. For example, the effective dose of colchicine is similar to the dose that produces diarrhea and other gastrointestinal symptoms. Absolutely contraindicated in the case of bleeding, and the administration of phenylbutazone for as short as 3 weeks can also cause severe neutropenia or aplastic anemia

Method used

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  • Composition and application thereof in drug for resisting acute gout
  • Composition and application thereof in drug for resisting acute gout
  • Composition and application thereof in drug for resisting acute gout

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0016] The preparation of embodiment 1 compound Schiglautone A

[0017] The preparation method of the compound Schiglautone A (I) refers to the method published by Fan-Yu Mengetal.

[0018]

Embodiment 2

[0019] The synthesis of the O-bromoethyl derivative (II) of embodiment 2SchiglautoneA

[0020] Compound I (502 mg, 1.00 mmol) was dissolved in 15 mL of benzene, and tetrabutylammonium bromide (TBAB) (0.08 g), 1,2-dibromoethane (7.520 g, 40.00 mmol) and 6 mL of 50% sodium hydroxide solution. The mixture was stirred at 35 °C for 8 h. After 8 hours, the reaction solution was poured into ice water, extracted twice with dichloromethane immediately, and the organic phase solutions were combined. Then the organic phase solution was washed with water and saturated brine three times successively, then dried with anhydrous sodium sulfate, and finally concentrated under reduced pressure to remove the solvent to obtain a crude product. The crude product was purified by silica gel column chromatography (mobile phase: petroleum ether / acetone=100:1.0, v / v), the brown concentrated elution band was collected and the solvent was evaporated to obtain a brown powder of Compound II (508mg, 71%) ...

Embodiment 3

[0025] The synthesis of the O-(diethylamino) ethyl derivative (III) of embodiment 3 Schiglautone A

[0026] Compound II (358mg, 0.5mmol) was dissolved in 10mL of acetonitrile, anhydrous potassium carbonate (690mg, 5.0mmol), potassium iodide (168mg, 1.0mmol) and diethylamine (2920mg, 40mmol) were added thereto, and the mixture was heated to reflux for 8h . After the reaction, the reaction solution was poured into ice water, extracted twice with an equal amount of dichloromethane, and the organic phases were combined. The combined organic phases were successively washed with water and saturated brine, dried over anhydrous sodium sulfate, and concentrated under reduced pressure to remove the solvent to obtain a crude product. The crude product was purified by silica gel column chromatography (mobile phase: petroleum ether / acetone=100:1.0, v / v), the brown concentrated elution band was collected and the solvent was evaporated to obtain a brown powder of compound III (231.2mg, 66% ...

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Abstract

The invention relates to the fields of organic synthesis and medicinal chemistry, and in particular relates to a composition, a preparation method and application of the composition in preparing a drug for resisting acute gout. The invention discloses a composition and a preparation method thereof. Based upon pharmacological experiments, the composition disclosed by the invention has an effect on resisting the acute gout, so that the composition has the value of developing the drug for resisting the acute gout.

Description

technical field [0001] The invention relates to the fields of organic synthesis and medicinal chemistry, in particular to a composition, a preparation method and an application thereof. Background technique [0002] Gout, also known as gouty arthritis, is a disease caused by the disorder of purine metabolism in the body. It is manifested by excessive uric acid in the blood, and it is easy to cause urate (MSU) to precipitate and crystallize in joints and other tissues. The acute attack of gout is due to the local neutrophil infiltration and inflammatory response caused by MSU deposited in the joints. [0003] Western medicine selects three kinds of medicines for use in the acute attack stage of gout: colchicine, non-steroidal anti-inflammatory drugs and corticosteroids. The mechanism of action of colchicine is to bind to the tubulin of neutrophils, thereby hindering the activity of granulocytes and inhibiting granulocyte infiltration. Non-steroidal anti-inflammatory drugs s...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/192A61P19/06C07C217/12
CPCA61K31/192C07C217/12
Inventor 江春平吴俊华
Owner NANJING GUANGKANGXIE BIOLOGICAL MEDICAL TECH
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