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Composition and application thereof to acute renal failure resistant drug

A technology of acute renal failure and composition, applied in the fields of organic synthesis and medicinal chemistry, to achieve the effect of improving function

Inactive Publication Date: 2016-03-09
NANJING UNIV
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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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  • Composition and application thereof to acute renal failure resistant drug
  • Composition and application thereof to acute renal failure resistant drug
  • Composition and application thereof to acute renal failure resistant drug

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0012] The preparation of embodiment 1 compound Schiglautone A

[0013] The preparation method of the compound Schiglautone A (I) refers to the method published by Fan-Yu Mengetal.

[0014]

Embodiment 2

[0015] The synthesis of the O-bromoethyl derivative (II) of embodiment 2SchiglautoneA

[0016] 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

[0021] Synthesis of O-(morpholinyl) ethyl derivative (III) of embodiment 3 Schiglautone A

[0022] Compound II (358 mg, 0.5 mmol) was dissolved in 20 mL of acetonitrile, anhydrous potassium carbonate (345 mg, 2.5 mmol), potassium iodide (168 mg, 1.0 mmol) and morpholine (3484 mg, 40 mmol) were added thereto, and the mixture was heated to reflux for 4 h. After the reaction was completed, the reaction solution was poured into 20 mL of 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=100:0.5, v / v), the yellow concentrated elution band was collected and the solvent was evaporated to obtain a brown powder of compou...

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Abstract

The invention relates to the field of organic synthesis and medicinal chemistry, in particular to a composition, a preparing method and application thereof to an acute renal failure resistant drug. The invention discloses the composition and the preparing method thereof. The pharmacology experiments show that the composition has an acute renal failure resistant function and has value of developing the acute renal failure resistant drug.

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] 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, with a high incidence and often serious consequences, characterized by short-term (hours to days) renal failure A sharp decline in function, clinical manifestations of acute oliguria (urine output <400mLPd) or anuria (urine output <100mLPd), obstruction of nitrogen metabolite excretion in the body, rapid occurrence of azotemia, disturbance of water, electrolyte, and acid-base balance , And cause the corresponding dysfunction of the various systems 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...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/5377A61K31/192A61P13/12C07D295/088C07C217/12
CPCA61K31/192A61K31/5377C07C217/12C07D295/088A61K2300/00
Inventor 吴俊华周未末
Owner NANJING UNIV