Composition 38083001030527 and application of composition 38083001030527 to drug for resisting 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: 2015-11-25
苏州贺澳德生物医药科技有限公司
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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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  • Composition 38083001030527 and application of composition 38083001030527 to drug for resisting acute gout
  • Composition 38083001030527 and application of composition 38083001030527 to drug for resisting acute gout
  • Composition 38083001030527 and application of composition 38083001030527 to drug for resisting acute gout

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Experimental program
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Embodiment 1

[0016] The preparation of embodiment 1 compound PsiguadialA

[0017] The preparation method of the compound PsiguadialA (I) refers to the method published by Meng Shao et al. (Meng Shao et al., 2010. Psiguadials A and B, Two Novel Meroterpenoids with Unusual Skeletons from the Leaves of Psidiumguajava. Organic Letters 12 (2010) 5040-5043).

[0018]

Embodiment 2

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

[0020] Compound I (474 ​​mg, 1.00 mmol) was dissolved in 20 mL of benzene, tetrabutylammonium bromide (TBAB) (0.16 g), 1,2-dibromoethane (7.520 g, 40.00 mmol) and 12 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=100:0.5, v / v), the brown concentrated elution band was collected and the solvent was evaporated to obtain a brown powder of Compound II (502mg, 73%) . ...

Embodiment 3

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

[0026] Compound II (344mg, 0.5mmol) was dissolved in 20mL 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 9h . After the reaction, the reaction solution was poured into ice water, extracted 4 times 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=100:1.5, v / v), the yellow concentrated elution band was collected and the solvent was evaporated to obtain a yellow powder of compound III (231.8mg, 69% ...

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Abstract

The invention relates to the fields of organic synthesis and medicinal chemistry, in particular to a composition 38083001030527, a preparation method of the composition 38083001030527, and application of the composition 38083001030527 to a drug for resisting acute gout, and discloses the composition 38083001030527 and the preparation method. Pharmacological experiments show that the composition 38083001030527 plays a role in resisting acute gout, thereby having a high value on development of the drug for resisting acute gout.

Description

technical field [0001] The present invention relates to the fields of organic synthesis and medicinal chemistry, in particular to composition 38083001030527, a preparation method and its use. 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 d...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/4545A61P19/06C07D313/06A61K31/335
Inventor 朱磊磊
Owner 苏州贺澳德生物医药科技有限公司
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