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Application of diethylamine derivative of Cleistanone in preparation of medicine resistant to acute renal failure

A kind of technology of closing floridone and acute renal failure, which is applied in the direction of drug combination, medical preparation containing active ingredients, medical formula, etc., to achieve the effect of obvious therapeutic effect.

Active Publication Date: 2014-10-15
SHANDONG UNIV QILU HOSPITAL
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

There are few clinical drugs that have obvious effects on improving renal blood perfusion disorder and reducing renal tissue damage

Method used

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  • Application of diethylamine derivative of Cleistanone in preparation of medicine resistant to acute renal failure
  • Application of diethylamine derivative of Cleistanone in preparation of medicine resistant to acute renal failure
  • Application of diethylamine derivative of Cleistanone in preparation of medicine resistant to acute renal failure

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0019] Preparation of Example 1 Compound Cleistanone

[0020] The preparation method of the compound Cleistanone (I) refers to the literature published by Van Trinh Thi Thanh et al. , pages 4108–4111, August 2011).

[0021]

Embodiment 2

[0022] Synthesis of O-bromoethyl derivatives (II) of cleistanone Cleistanone of embodiment 2

[0023] Compound I (440 mg, 1.00 mmol) was dissolved in 10 mL of benzene, and tetrabutylammonium bromide (TBAB) (0.04 g), 1,2-dibromoethane (3.760 g, 20.00 mmol) and 6 mL of 50% sodium hydroxide solution. The mixture was stirred at 25 °C for 24 h. After 24 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, v / v), and the yellow concentrated elution band was collected to obtain compound II as a yellow solid (344 mg, 63%).

[0024] 1H NMR ...

Embodiment 3

[0028] Example 3 Synthesis of O-(diethylamino)ethyl derivatives (III) of Cleistanone

[0029] Compound II (273mg, 0.5mmol) was dissolved in 20mL of acetonitrile, anhydrous potassium carbonate (345mg, 2.5mmol), potassium iodide (84mg, 0.5mmol) and diethylamine (1460mg, 20mmol) were added thereto, and the mixture was heated to reflux for 8h . After the reaction was completed, 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 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, v / v), and the light yellow concentrated elution band was collected to obtain compound III as a light yellow colloidal solid (169.8mg, 63% ...

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Abstract

The invention relates to the fields of organic synthesis and medicinal chemistry and particularly to a derivative of Cleistanone, the preparation method for the derivative of the Cleistanone and the usage of the derivative of Cleistanone in preparing medicine resistant to acute renal failure. According to the invention, a novel derivative of the Cleistanone is synthesized and the preparation method for the novel derivative of the Cleistanone is disclosed. Pharmacological experiments indicate that the derivative of the Cleistanone provided by the invention has the function of resisting the acute renal failure and has the value of developing medicine resistant to the acute renal failure.

Description

technical field [0001] The present invention relates to the fields of organic synthesis and medicinal chemistry, in particular to a Cleistanone derivative, a preparation method and an application thereof. Background technique [0002] Acute renal failure (Acute Renal Failure, ARF) is a clinical syndrome caused by a variety of reasons, which can be seen in patients of various clinical departments. It has a high incidence and often brings serious consequences. ) with a sharp decline in renal function, clinical manifestations of acute oliguria (urine output <400mLPd) or anuria (urine output <100mLPd), obstacles in the excretion of nitrogen metabolites in the body, rapid azotemia, water and electrolytes, acid-base Balance disorder, and cause the corresponding dysfunction of the system of the whole body. The main factors causing acute renal failure are the sharp reduction of renal blood flow, as well as the oxidative stress and cell damage caused by renal tissue ischemia, ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/56A61P13/12C07J63/00
Inventor 罗东君吴俊艺黄蓉吴俊华
Owner SHANDONG UNIV QILU HOSPITAL
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