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Flurbiprofen chalcone compound as well as preparation method and application thereof

A ketone compound and compound technology are applied to a class of flurbiprofen chalcone compounds, their preparation and application fields, and can solve the problems of single action target, many toxic and side effects, and poor long-term efficacy in AD patients.

Active Publication Date: 2018-06-01
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 compound as well as preparation method and application thereof
  • Flurbiprofen chalcone compound as well as preparation method and application thereof
  • Flurbiprofen chalcone compound as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] Embodiment 1 General method for the preparation of flurbiprofen chalcones (I)

[0036] Add 2.0 mmol of the corresponding 3′-acetyl-4′-hydroxyflurbiprofen compound (2), 3.0 mmol of the corresponding aromatic formaldehyde compound (1), 8.0 mmol of anhydrous potassium carbonate and 50 ml Acetonitrile, 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, cool to room temperature, adjust the pH of the reaction solution to strong acidity with 10% hydrochloric acid aqueous solution, and then use saturated aqueous sodium bicarbonate solution Adjust the pH of the reaction solution to weak alkalinity, distill off acetonitrile under reduced pressure, add 50 mL of deionized water to the residual liquid, and extract it three times with 150 mL of dichloromethane. After drying with sodium sulfate and filtering, the solvent was evaporated under reduced pressure, and the residue was purified by silica gel ...

Embodiment 2

[0086] Example 2 General method for preparation of flurbiprofen chalcone compound (I) and acid salt formation

[0087] Add the flurbiprofen-chalcone compound (I) (that is: R 1 and R 2 Each independently represents NR 4 R 5 1.0 mmol of acetone) and 20 ml of acetone, stirred evenly, added 3.0 mmol of the corresponding acid, heated and refluxed and stirred for 20 minutes, cooled to room temperature after the reaction, evaporated the solvent under reduced pressure, recrystallized the residue by conventional methods, filtered The solid that separates out promptly obtains the salt of corresponding flurbiprofen-chalcone compound (I), and its chemical structure 1 Confirmed by H NMR and ESI-MS.

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Abstract

The invention discloses a novel flurbiprofen chalcone compound (I), pharmaceutically acceptable salt thereof, a preparation method thereof, a pharmaceutical composition and application to preparationof drugs for treating and / or preventing diseases related to neurodegeneration, including but not limited to neurodegeneration diseases of vascular dementia, an Alzheimer's disease, a Parkinson's disease, a Huntington's disease, HIV-related dementia, MS (multiple sclerosis), progressive lateral sclerosis 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 new type of flurbiprofen chalcone compound (I) and its pharmaceutically acceptable salt, its preparation method, pharmaceutical composition and preparation for treating and / or preventing neurodegeneration Sex-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, neurological Pain, glaucoma and other neurodegenerative diseases. 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 United States. According to th...

Claims

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Application Information

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IPC IPC(8): C07C59/90C07C229/42C07D295/155C07D211/14C07D333/24C07D307/56C07D307/54C07D333/28C07D333/32C07D213/64C07D213/50C07C235/78C07C69/738A61K31/216A61K31/402A61K31/4453A61K31/451A61K31/496A61K31/5375A61P25/00A61P25/28A61P25/16A61P31/18A61P25/14A61P25/04A61P27/06C07C51/353C07C227/26
CPCC07C59/90C07C69/738C07C229/42C07C235/78C07D211/14C07D213/50C07D213/64C07D295/155C07D307/54C07D307/56C07D333/24C07D333/28C07D333/32
Inventor 邓勇谭正怀杨杰宋青田超全杨子仪李维
Owner SICHUAN UNIV
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