Composition 77092202050623 and application thereof in anti-hepatic fibrosis drugs

A liver fibrosis and composition technology, applied in the fields of organic synthesis and medicinal chemistry, can solve the problems of lack of clinical treatment methods

Inactive Publication Date: 2016-01-20
CHANGZHOU HIGH TECH RES INST OF NANJING UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

In recent years, some anti-hepatic fibrosis treatments have emerged, including chemical drugs, biological agents, traditional Chinese medicine and gene therapy, etc., but the ideal clinical treatment methods are still lacking (Liu Ping. Strengthen the research on the mechanism of anti-hepatic fibrosis. Chinese liver disease Magazine, 2005, 8(13): 561)

Method used

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  • Composition 77092202050623 and application thereof in anti-hepatic fibrosis drugs
  • Composition 77092202050623 and application thereof in anti-hepatic fibrosis drugs
  • Composition 77092202050623 and application thereof in anti-hepatic fibrosis drugs

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0015] The preparation of embodiment 1 compound Schiglautone A

[0016] The preparation method of the compound Schiglautone A (I) refers to the method published by Fan-Yu Mengetal.

[0017]

Embodiment 2

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

[0019] 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

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

[0025] Compound II (358 mg, 0.5 mmol) was dissolved in 15 mL of acetonitrile, anhydrous potassium carbonate (690 mg, 5.0 mmol), potassium iodide (168 mg, 1.0 mmol) and pyrrolidine (2840 mg, 40 mmol) were added thereto, and the mixture was heated to reflux for 6 h. 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 brown concentrated elution band was collected and the solvent was evaporated to obtain a brown powder of compound III...

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Abstract

The invention relates to the fields of organic synthesis and medicinal chemistry, in particular to a composition 77092202050623, a preparing method of the composition 77092202050623 and the application of the composition 77092202050623 in preparing anti-hepatic fibrosis drugs. Pharmacology experiments show that the composition 77092202050623 can resist hepatic fibrosis and can be used for developing anti-hepatic fibrosis drugs.

Description

technical field [0001] The present invention relates to the fields of organic synthesis and medicinal chemistry, in particular to composition 77092202050623, preparation method and application thereof. Background technique [0002] Liver fibrosis is a dynamic process from chronic liver injury to liver cirrhosis, manifested in the synthesis and secretion of a large amount of extracellular matrix (ECM), while the degradation is absolutely or relatively insufficient, resulting in the diffuse deposition of ECM in the liver. It starts with necrosis of hepatocytes (HC), followed by inflammatory response, release of fibrogenesis mediators, activation of hepatic stellate cells (FSC), and finally, the synthesis and degradation of liver connective tissue components are obviously out of balance. Liver fibrosis is a common pathological process of many chronic liver diseases and an important factor affecting prognosis. [0003] In the past 20 years, the study of liver fibrosis has made ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/496A61P1/16A61K31/4025
Inventor 华子春吴俊华黄蓉王慧
Owner CHANGZHOU HIGH TECH RES INST OF NANJING UNIV
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