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Application of Atropurpuran derivative composition in anti-inflammation drugs

A composition and drug technology, which can be used in drug combinations, anti-inflammatory agents, active ingredients of heterocyclic compounds, etc., and can solve the problems of high toxicity and low safety.

Inactive Publication Date: 2017-02-22
NANJING FUHAIAOSAI PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0003] The existing drugs for the treatment of inflammation have the problems of high toxicity and low safety. It is of great value to find compounds or lead compounds from natural products and carry out structural modification to obtain their derivatives, so as to obtain potential drugs with high efficiency and low toxicity

Method used

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  • Application of Atropurpuran derivative composition in anti-inflammation drugs
  • Application of Atropurpuran derivative composition in anti-inflammation drugs
  • Application of Atropurpuran derivative composition in anti-inflammation drugs

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Experimental program
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Effect test

Embodiment 1

[0015] The preparation of embodiment 1 compound Atropurpuran

[0016] The preparation method of 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.Tetrahedron Letters50(2009)460-462 )Methods.

[0017]

Embodiment 2

[0018] The synthesis of the O-bromoethyl derivative (II) of embodiment 2 Atropurpuran

[0019] Compound I (312 mg, 1.00 mmol) was dissolved in 10 mL of benzene, 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 °C for 6 h. After 6h, 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 yellow powder of Compound II (309mg, 74%) .

[0...

Embodiment 3

[0024] The synthesis of O-(tetrahydropyrrolyl) ethyl derivative (III) of embodiment 3 Atropurpuran

[0025] Compound II (209 mg, 0.5 mmol) was dissolved in 18 mL of acetonitrile, anhydrous potassium carbonate (345 mg, 2.5 mmol), potassium iodide (84 mg, 0.5 mmol) and pyrrolidine (1420 mg, 20 mmol) were added thereto, and the mixture was heated to reflux for 2 h. 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), and the concentrated brown elution band was collected and concentrated to give compound III as a brown solid (125 mg, 61%).

[00...

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Abstract

The invention discloses an application of an Atropurpuran derivative composition in anti-inflammation drugs, relates to the field of organic synthesis and medicinal chemistry and particularly relates to a composition, a preparation method and an application of the composition in preparing anti-inflammation drugs. The invention discloses the composition and the preparation method thereof. Pharmacological experiments indicate that the composition disclosed by the invention has an anti-inflammation effect and a value in developing anti-inflammation drugs.

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] Inflammation occurs locally but can also affect the whole body. Local clinical features are redness, heat, swelling, pain and dysfunction. Redness and heat are due to the expansion of local blood vessels and the acceleration of blood flow due to inflammation. Swelling is caused by local inflammatory hyperemia and exudation of blood flow components. The development of drugs with anti-inflammatory effects is of great significance for the verification of relief and pain relief. [0003] The existing drugs for the treatment of inflammation have the problems of high toxicity and low safety. It is of great value to find compounds or lead compounds from natural products and carry out structural modification to obtain their derivatives, so as to obtain potential drugs...

Claims

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Application Information

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IPC IPC(8): A61K31/41A61K31/40C07D257/04C07D295/088A61P29/00
CPCA61K31/41A61K31/40C07D257/04C07D295/088
Inventor 王卓婷
Owner NANJING FUHAIAOSAI PHARMA CO LTD
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