2,5-dyhydroxy-p-phthalamide compound and preparation method and application thereof

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 poor long-term curative effect and single action target of AD patients , many toxic and side effects

Active Publication Date: 2019-01-25
SICHUAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, these drugs have problems such as a single target, more toxic and si

Method used

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  • 2,5-dyhydroxy-p-phthalamide compound and preparation method and application thereof
  • 2,5-dyhydroxy-p-phthalamide compound and preparation method and application thereof
  • 2,5-dyhydroxy-p-phthalamide compound and preparation method and application thereof

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 2.0mmol of 2,5-dihydroxyterephthalamide compound (I) obtained according to the above-mentioned Example 1 and 35ml of acetone into the reaction flask, stir evenly, add 6.0mmol of the corresponding acid, heat up and reflux and stir for 20 Minutes, after the completion of the reaction, 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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Abstract

The invention discloses a novel 2,5-dyhydroxy-p-phthalamide compound (I) and pharmaceutically acceptable salts thereof, a preparation method of the compound and application in preparing medicine treating and/or preventing nervous system related diseases. The diseases include but not limited to the vascular dementia, presenile dementia, Parkinson's disease, Huntington's disease, HIV related Alzheimer disease, nerve injuries caused by the traumatic brain injury and other diseases. The formula is defined in the description.

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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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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