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Composition 64083001030526 and application thereof in acute renal failure resisting medicine

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

Inactive Publication Date: 2015-11-11
苏州贺澳德生物医药科技有限公司
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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 64083001030526 and application thereof in acute renal failure resisting medicine
  • Composition 64083001030526 and application thereof in acute renal failure resisting medicine
  • Composition 64083001030526 and application thereof in acute renal failure resisting medicine

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0012] The preparation of embodiment 1 compound PsiguadialA

[0013] 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).

[0014]

Embodiment 2

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

[0016] 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

[0021] The synthesis of the O-(diethylamino) ethyl derivative (III) of embodiment 3PsiguadialA

[0022] 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 field of organic synthesis and medicinal chemistry, in particular to a composition 64083001030526, a preparation method and an application thereof in preparing acute renal failure resisting medicine, and discloses the composition 64083001030526 and the preparation method thereof. Pharmacology experiments prove that the composition 64083001030526 has the function of resisting acute renal failure and has the value of developing the acute renal failure resisting medicine.

Description

technical field [0001] The present invention relates to the fields of organic synthesis and medicinal chemistry, in particular to composition 64083001030526, a preparation method and its application. 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 s...

Claims

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Application Information

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IPC IPC(8): A61K31/4523A61P13/12A61K31/335
Inventor 朱磊磊
Owner 苏州贺澳德生物医药科技有限公司