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A class of 2,5-dihydroxyterephthalamide compounds, its preparation method and use

A technology of hydroxyterephthalamide and compounds, which is applied in a class of 2,5-dihydroxyterephthalamide compounds, their preparation and application fields, and can solve the problem of single action target, many toxic and side effects, and AD patients Poor long-term efficacy and other issues

Active Publication Date: 2021-04-27
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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  • A class of 2,5-dihydroxyterephthalamide compounds, its preparation method and use
  • A class of 2,5-dihydroxyterephthalamide compounds, its preparation method and use
  • A class of 2,5-dihydroxyterephthalamide compounds, its preparation method and use

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] Example 1 General method for the preparation of 2,5-dihydroxyterephthalamide compounds (I)

[0037] Add 3.0 mmol of 2,5-dihydroxyterephthalic acid (1), 9.0 mmol of the corresponding primary amine compound (2) and 15 ml of tetrahydrofuran in sequence in the reaction flask, stir well at room temperature and then add 1-ethyl-3- (3-Dimethylaminopropyl) carbodiimide hydrochloride 9.0 mmol and triethylamine 12.0 mmol, continue stirring at room temperature for 10 to 32 hours (reaction progress tracked by TLC). After the reaction was completed, the solvent was evaporated under reduced pressure, 40 mL of dichloromethane was added to the residue, and 20 mL of deionized water, 20 mL of saturated NaHCO 3 aqueous solution and 20 mL saturated NaCl aqueous solution, the organic layer was dried over anhydrous sodium sulfate and filtered, the solvent was distilled off under reduced pressure, and the residue was purified by silica gel column chromatography (eluent: acetone:dichloromethan...

Embodiment 2

[0064] Example 2 General method for the preparation of 2,5-dihydroxyterephthalamide compound (I) and acid salt formation

[0065] Add 2.0 mmol of the 2,5-dihydroxyterephthalamide compound (I) obtained in the above-mentioned Example 1 and 35 ml of acetone into the reaction flask, stir evenly, add 6.0 mmol of the corresponding acid, and heat up to reflux and stir for 20 Minutes, after the reaction is completed, cool to room temperature, evaporate the solvent under reduced pressure, and recrystallize the residue to obtain the salt of 2,5-dihydroxyterephthalamide compound (I) and acid. 1 Confirmed by H NMR and ESI-MS.

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PUM

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Abstract

The invention discloses a class of 2,5-dihydroxyterephthalamide compounds (I) and pharmaceutically acceptable salts thereof, their preparation methods, pharmaceutical compositions and preparations for treating and / or preventing nervous system-related diseases Use in pharmaceuticals, including but not limited to vascular dementia, Alzheimer's disease, Parkinson's disease, Huntington's disease, HIV-related dementia, multiple sclerosis, amyotrophic lateral sclerosis, neuropathic pain, Glaucoma, ischemic stroke, hemorrhagic stroke, and neurological damage caused by traumatic brain injury;

Description

technical field [0001] The invention belongs to the field of medicinal chemistry, and relates to a novel 2,5-dihydroxyterephthalamide compound (I), its preparation method, pharmaceutical composition and preparation of medicines for treating and / or preventing nervous system-related diseases including, but not limited to, vascular dementia, Alzheimer's disease, Parkinson's disease, Huntington's disease, HIV-related dementia, multiple sclerosis, amyotrophic lateral sclerosis, neuropathic pain, glaucoma, Ischemic stroke, hemorrhagic stroke, and neurological damage caused by traumatic brain injury. Background technique [0002] Neurodegenerative diseases refer to the general term for diseases caused by chronic progressive degeneration of central nervous tissue, including Alzheimer's disease (Alzheimer's disease, AD), Parkinson's disease (Parkinson's disease, PD), Huntington's disease (Huntington disease, HD), amyotrophic lateral sclerosis (Amyotrophic lateral sclerosis, ALS) and...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07C235/60C07C231/02C07D211/26C07D295/13C07D211/14A61P9/10A61P25/28A61P25/14A61P31/18A61P25/04A61P27/06A61P25/16A61K31/165A61K31/445A61K31/495A61K31/5375A61K31/4453A61K31/40
CPCA61P9/10A61P25/04A61P25/14A61P25/16A61P25/28A61P27/06A61P31/18C07C231/02C07C235/60C07D211/14C07D211/26C07D295/13
Inventor 邓勇李岩宋青田超全杨子仪李维
Owner SICHUAN UNIV
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