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Flurbiprofen chalcone mannich base compounds as well as preparation method and application thereof

A technology of keto Mannich base and hydroxybenzaldehyde Mannich base, which is applied in the fields of flurbiprofen-chalcone Mannich base compounds, their preparation and application, and can solve the problem of single target and long-term treatment of AD patients. Poor curative effect, many side effects and other problems

Active Publication Date: 2019-07-12
SICHUAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, these drugs have problems such as a single target, more toxic and side effects in clinical use, and poor long-term curative effect on AD patients.

Method used

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  • Flurbiprofen chalcone mannich base compounds as well as preparation method and application thereof
  • Flurbiprofen chalcone mannich base compounds as well as preparation method and application thereof
  • Flurbiprofen chalcone mannich base compounds as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] Example 1 General method for the preparation of flurbiprofen-chalcone Mannich base compound (I)

[0036]Add 2.0 mmol of the corresponding 4′-acetylflurbiprofen compound (1), 3.0 mmol of the corresponding hydroxybenzaldehyde Mannich base compound (2), 8.0 mmol of anhydrous potassium carbonate and 50 ml of acetonitrile into the reaction flask , after stirring evenly, heat up and reflux and stir for 2.0 to 72.0 hours (the reaction process is tracked by TLC); after the reaction is completed, cool to room temperature, adjust the pH of the reaction solution to strong acidity with 10% hydrochloric acid aqueous solution, and then adjust it with saturated sodium bicarbonate aqueous solution The pH of the reaction solution was slightly alkaline, acetonitrile was evaporated under reduced pressure, 50 mL of deionized water was added to the residual liquid, extracted three times with 150 mL of dichloromethane, the organic layers were combined, washed with saturated aqueous sodium chl...

Embodiment 2

[0056] Example 2 General method for the preparation of flurbiprofen-chalcone Mannich base compound (I) and acid salt formation

[0057] Add 2.0 mmol of the flurbiprofen-chalcone Mannich base compound (I) obtained in the above-mentioned Example 1 and 50 ml of acetone into the reaction flask, stir evenly, add 5.0 mmol of the corresponding acid, heat up and reflux and stir for 20 Minutes, after the reaction is finished, cool to room temperature, evaporate the solvent under reduced pressure, and the residue is recrystallized by a conventional method, and the precipitated solid is filtered to obtain the salt of flurbiprofen-chalcone Mannich base compound (I), which chemical structure 1 Confirmed by H NMR and ESI-MS.

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Abstract

The invention discloses novel flurbiprofen chalcone mannich base compounds (I) and pharmaceutically acceptable salts thereof, a preparation method of the compounds, pharmaceutical composition and an application in preparation of drugs for treating and / or preventing neurodegeneration related diseases including but not limited to vascular dementia, Alzheimer's disease, Parkinson's disease, Huntington disease, HIV related dementia, multiple sclerosis, progressive lateral sclerosis of spinal cord, neuropathic pain, glaucoma and the like.

Description

technical field [0001] The invention belongs to the field of medicinal chemistry, and relates to a novel flurbiprofen-chalcone Mannich base compound (I) and a pharmaceutically acceptable salt thereof, a preparation method thereof, a pharmaceutical composition and preparation methods for treating and / or or prevention of neurodegenerative related diseases, including but not limited to vascular dementia, Alzheimer's disease, Parkinson's disease, Huntington's disease, HIV-related dementia, multiple sclerosis, progressive lateral sclerosis Neurodegenerative diseases such as neuropathic pain and glaucoma. Background technique [0002] Alzheimer's disease (Alzheimer's disease, AD, senile dementia) is a degenerative disease of the central nervous system mainly characterized by progressive cognitive impairment and memory impairment. Vascular diseases and cancers are high-incidence diseases, which have risen to the fourth cause of death in developed countries such as Europe and the U...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C229/34C07C227/16C07C237/20C07C231/12C07D295/155A61K31/216A61K31/40A61K31/4453A61K31/5375A61K31/495A61K31/165A61P25/28A61P25/16A61P25/14A61P31/18A61P27/06A61P25/04A61P9/10
CPCC07C229/34C07C237/20C07D295/155
Inventor 邓勇强晓明宋青田超全杨子仪李维
Owner SICHUAN UNIV
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