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Tetrahydroisoquinoline compound and preparation method and application thereof

A technology of tetrahydroisoquinoline and compounds, which is applied in the field of medicine, can solve problems such as memory loss, and achieve the effects of low toxicity, good clinical application prospects, and low cost

Inactive Publication Date: 2017-06-13
NANYANG NORMAL UNIV
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Problems solved by technology

However, the above-mentioned patents mainly focus on the research on nerve cell damage caused by oxidative stress. Oxidative stress is an intermediate link in the development of AD, which may be caused by factors such as excessive metal ion disorder or β-amyloid deposition. It shows that the lack of acetylcholine level in the brain of AD patients is the main cause of memory loss in AD patients. The enzymes that hydrolyze acetylcholine mainly include acetylcholinesterase and butyrylcholinesterase. With the development of AD, acetylcholinesterase (AChE) The level gradually decreased, while the activity of butyrylcholinesterase (BuChE) increased to 165% of the normal value, while the above-mentioned patent had no inhibitory activity on cholinesterase

Method used

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  • Tetrahydroisoquinoline compound and preparation method and application thereof
  • Tetrahydroisoquinoline compound and preparation method and application thereof
  • Tetrahydroisoquinoline compound and preparation method and application thereof

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Embodiment 1

[0032] A 3,4-dihydro-2(1H)-quinolinone-7-O-alkyl-1,2,3,4-tetrahydroisoquinoline compound, the general chemical structure of which is shown in I:

[0033]

[0034] where n=3.

[0035] The preparation method of the above-mentioned 3,4-dihydro-2(1H)-quinolinone-7-O-alkyl-1,2,3,4-tetrahydroisoquinoline compound comprises the following steps:

[0036] 3,4-dihydro-7 hydroxy-2 (1H)-quinolinone 1 (1mmol), K 2 CO 3 (1.2mmol) and anhydrous acetonitrile were added to the reaction flask, after stirring evenly, dibromide 2 (2.2mmol) was added, after the addition was completed, stirred at 65°C for 6h, monitored by TLC; after the reaction was completed, the solvent was evaporated under reduced pressure, and the residue was Add water (40mL), extract with dichloromethane (40mL×2), combine the organic layers and wash with saturated aqueous sodium chloride solution (40mL), dry over anhydrous sodium sulfate, filter, and distill the filtrate to remove the solvent under reduced pressure, and t...

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Abstract

The invention belongs to the technical field of medicines, in particular to a 3, 4-dihydro-2(1H)-quinolinone-7-O-alkyl-1, 2, 3, 4-tetrahydroisoquinoline compound and a preparation method and application thereof. The compound has the chemical structural general formula shown as a formula I. The compound has an inhibitory effect on butyrylcholinesterase, acetylcholinesterase, MAO-A and MAO-B, and has a selective inhibitory effect on butyrylcholinesterase, is a multi-target inhibitor, and further shows a better therapeutic effect on Alzheimer's disease in an in-vivo experiment, has low toxicity, and has a very good clinical application prospect.

Description

technical field [0001] The invention belongs to the technical field of medicine, and specifically relates to a 3,4-dihydro-2(1H)-quinolinone-7-O-alkyl-1,2,3,4-tetrahydroisoquinoline compound and its Preparation method and use. Background technique [0002] Alzheimer's disease (Alzheimer's disease, AD, senile dementia) is a central nervous system degenerative disease mainly characterized by progressive cognitive impairment and memory impairment. With the rapid aging of the global population, the elderly population Health problems have become a major social problem that needs to be solved urgently. Alzheimer's disease (AD) is one of the diseases with the highest morbidity and mortality among the elderly. According to the "2015 Global Alzheimer's Report" released by Alzheimer's Disease International (ADI), more than 46 million people in the world suffered from dementia in 2015. It is predicted that by 2050, the world's There will be 131.5 million people suffering from dement...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D401/12A61K31/4725A61P25/28
CPCC07D401/12
Inventor 桑志培王柯人柳文敏潘万里马勤阁孙丽红
Owner NANYANG NORMAL UNIV
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