Composition 67083001030512 and application of composition 67083001030512 to drug for resisting liver fibrosis

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: 2015-11-25
苏州贺澳德生物医药科技有限公司
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  • 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 id

Method used

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  • Composition 67083001030512 and application of composition 67083001030512 to drug for resisting liver fibrosis
  • Composition 67083001030512 and application of composition 67083001030512 to drug for resisting liver fibrosis
  • Composition 67083001030512 and application of composition 67083001030512 to drug for resisting liver fibrosis

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Experimental program
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Effect test

Embodiment 1

[0015] The preparation of embodiment 1 compound PsiguadialA

[0016] 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).

[0017]

[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 67083001030512, a preparation method of the composition 67083001030512, and application of the composition 67083001030512 to a drug for resisting liver fibrosis, and discloses the composition 67083001030512 and the preparation method. Pharmacological experiments show that the composition 67083001030512 plays a role in resisting liver fibrosis, thereby having a high value on development of the drug for resisting liver fibrosis.

Description

technical field [0001] The present invention relates to the fields of organic synthesis and medicinal chemistry, in particular to composition 67083001030512, a preparation method and its application. 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 gr...

Claims

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Application Information

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IPC IPC(8): A61K31/4545A61P1/16A61K31/335
Inventor 朱磊磊
Owner 苏州贺澳德生物医药科技有限公司
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