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Application of composition of imidazolyl and diethylamine chloride derivatives of Atropurpuran to resistance of acute gout

A technology of acute gout and composition, which is applied in the field of organic synthesis and medicinal chemistry, and can solve problems such as granulocytopenia and aplastic anemia

Inactive Publication Date: 2017-06-13
NANJING FUHAIAOSAI PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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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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  • Application of composition of imidazolyl and diethylamine chloride derivatives of Atropurpuran to resistance of acute gout
  • Application of composition of imidazolyl and diethylamine chloride derivatives of Atropurpuran to resistance of acute gout
  • Application of composition of imidazolyl and diethylamine chloride derivatives of Atropurpuran to resistance of acute gout

Examples

Experimental program
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Effect test

Embodiment 1

[0016] Example 1 Preparation of compound Atropurpuran

[0017] The preparation method of the compound Atropurpuran (I) refers to the literature published by Pei Tang et al. (Pei Tang et al., 2009. Atropurpuran, a novel diterpene with an unprecedented pentacycliccage skeleton, from Aconitum hemsleyanum var. atropurpureum. )Methods.

[0018]

Embodiment 2

[0019] Example 2 Synthesis of O-bromoethyl derivative (II) of Atropurpuran

[0020] Compound I (312 mg, 1.00 mmol) was dissolved in 10 mL of benzene, and to the solution was added tetrabutylammonium bromide (TBAB) (0.08 g), 1,2-dibromoethane (3.760 g, 20.00 mmol) and 6 mL of 50% sodium hydroxide solution. The mixture was stirred at 35 degrees Celsius for 6 h. After 6 h, the reaction solution was poured into ice water, immediately extracted twice with dichloromethane, and the organic phase solutions were combined. Then, the organic phase solution was washed with water and saturated brine three times in turn, dried over 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 bands were collected and the solvent was evaporated to obtain a yellow powder of compoun...

Embodiment 3

[0025] Example 3 Synthesis of O-(imidazolyl)ethyl derivative (III) of Atropurpuran

[0026] Compound II (209 mg, 0.5 mmol) was dissolved in 12 mL of acetonitrile, anhydrous potassium carbonate (345 mg, 2.5 mmol), potassium iodide (84 mg, 0.5 mmol) and imidazole (3480 mg, 40 mmol) were added thereto, and the mixture was heated to reflux for 4 h. After the reaction, the reaction solution was poured into ice water, extracted three times with an equal amount of dichloromethane, and the organic phases were combined. The combined organic phases were washed successively 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=100:0.7, v / v), and the brown concentrated elution bands were collected and concentrated to obtain compound III as a brown solid (156 mg, 77%).

[0027] 1H ...

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Abstract

The invention discloses application of a composition of imidazolyl and diethylamine chloride derivatives of Atropurpuran to resistance of acute gout, namely, application of a composition of an O-(imidazolyl)ethyl derivative and an O-(diethylamine chloride)ethyl derivative of the Atropurpuran to an acute gout resistant medicament. The invention relates to the fields of organic synthesis and pharmaceutical chemistry, in particular to a composition of Atropurpuran derivatives, a preparation method of the composition and application of the composition to preparation of the acute gout resistant medicament. The invention discloses a composition of Atropurpuran derivatives and a preparation method thereof. As proved by a pharmacology experiment, the composition of the Atropurpuran derivatives has the effect of resisting acute gout, and has a value of developing the acute gout resistant medicament.

Description

technical field [0001] The present invention relates to the fields of organic synthesis and medicinal chemistry, in particular to compositions, preparation methods and uses thereof. Background technique [0002] Gout (gouty), also known as gouty arthritis (gouty arthritis), is a disease caused by the disorder of purine metabolism in the body. The acute attack of gout is due to the local infiltration of neutrophils and inflammatory response caused by MSU deposited in the joints. [0003] Western medicine uses three kinds of drugs in the acute attack of gout: colchicine, non-steroidal anti-inflammatory drugs and adrenocortical hormones. The mechanism of action of colchicine is to bind to the tubulin of neutrophils, thereby hindering the activity of granulocytes and inhibiting the infiltration of granulocytes. Non-steroidal anti-inflammatory drugs such as indomethacin, inhibit cyclooxygenase (COX) activity and exert anti-inflammatory effects, and selective COX2 inhibitors. A...

Claims

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Application Information

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IPC IPC(8): A61K31/4164A61K31/13C07D233/60C07C217/12A61P19/06
CPCA61K31/4164A61K31/13C07C217/12C07D233/60
Inventor 王卓婷
Owner NANJING FUHAIAOSAI PHARMA CO LTD
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