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(E)-3-heteroaromatic propyl-2-enoic acid derivative as well as preparation and application thereof
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A technology of alkyl and medicine, which is applied in the field of (E)-3-aryl heterocyclyl prop-2-enoic acid derivatives and their preparation and application, and can solve any problems such as
Inactive Publication Date: 2020-08-25
MEDCURIUS INC
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Alzheimer's disease (AD) and Parkinson's disease (PD) are the two most common neurodegenerative diseases. Currently, there is no drug that can cure AD and PD, or even delay the progress of AD and PD. Some drugs for the treatment of AD and PD can only improve the symptoms of AD and PD patients
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Embodiment 1
[0046]
[0047] Steps: Put 0.298 g (2 mmol) of pyridine-2-acrylic acid (compound A) and 10 ml of methanol into the reaction flask, slowly add 0.03 g (0.3 mmol) of concentrated sulfuric acid dropwise, react at room temperature for 3 hours, add dropwise saturated carbonic acidSodiumhydrogen solution, adjust the pH to about 8, then extract with dichloromethane, dry over anhydrousmagnesiumsulfate, filter, concentrate, and dry to obtain 0.223 g of compound I-1, yield: 68%. 1 H NMR (CDCl 3 ): δ3.82(s, 3H), 6.95(d, 1H, J=16.0Hz), 7.28(m, 1H), 7.43(d, 1H, J=8.0Hz), 7.70(d, 1H, J= 16.0Hz), 7.73(m, 1H), 8.66(d, 1H, J=4.0Hz); MS(ESI): m / z 164[M+H] + .
Embodiment 2
[0049]
[0050] Steps: Put 0.298 g (2 mmol) of pyridine-2-acrylic acid (compound A) and 10 ml of ethanol into the reaction flask, slowly add 0.03 g (0.3 mmol) of concentrated sulfuric acid dropwise, react at room temperature for 3 hours, add saturated carbonic acid dropwise Sodiumhydrogen solution, adjust the pH to about 8, then extract with dichloromethane, dry over anhydrousmagnesiumsulfate, filter, concentrate, and dry to obtain 0.249 g of compound I-2, yield: 72%. 1 H NMR (CDCl 3 ): δ1.34(t, 3H, J=8.0Hz), 4.28(q, 2H, J=8.0Hz), 6.93(d, 1H, J=16.0Hz), 7.28(m, 1H), 7.44(d , 1H, J=8.0Hz), 7.69(d, 1H, J=16.0Hz), 7.73(m, 1H), 8.66(d, 1H, J=4.0Hz); MS(ESI): m / z 178[ M+H] + .
Embodiment 3
[0052]
[0053] Steps: put 0.298 g (2 mmol) of pyridine-3-acrylic acid (compound A) and 10 ml of methanol into the reaction flask, slowly add 0.03 g (0.3 mmol) of concentrated sulfuric acid, react at room temperature for 3 hours, add dropwise saturated carbonic acidSodiumhydrogen solution, adjust the pH to about 8, then extract with dichloromethane, dry over anhydrousmagnesiumsulfate, filter, concentrate, and dry to obtain 0.233 g of compound I-3, yield: 71%. 1 H NMR (CDCl 3 ): δ3.75 (s, 3H), 6.44 (d, 1H, J = 16.0Hz), 7.27 (dd, 1H, J = 4.0, 8.0Hz), 7.61 (d, 1H, J = 16.0Hz), 7.77 (d, 1H, J=8.0Hz), 8.54(d, 1H, J=4.0Hz), 8.67(s, 1H); MS(ESI): m / z 164[M+H] + .
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Abstract
The invention relates to a (E)-3-heteroaromatic propyl-2-enoic acid derivative, and also relates to a preparation method and pharmaceutical application thereof. The compound is a novel Nrf2 activatorand has the effects of resisting oxidative stress, resisting neuritis and enhancing mitochondrial functions and biogenesis by effectively activating an Nrf2 signal path, so that nerve cells are protected, and the compound can be used for treating neurodegenerative diseases and cerebral apoplexy. In addition, the novel Nrf2 activator can also be used to treat autoimmune diseases, diabetes and nephropathy, and other chronic diseases.
Description
technical field [0001] The present invention relates to a new class of Nrf2 activators, which can protect nerve cells by effectively activating the Nrf2 signaling pathway to produce anti-oxidative stress, anti-neuritis, and enhance mitochondrial function and biogenesis. For the treatment of multiple sclerosis (MS), Alzheimer's disease (AD), Parkinson's disease (PD), Huntington's disease (HD), amyotrophic lateral sclerosis (ALS), Friedreich's Ataxia (FRDA), spinal muscular atrophy (SMA), neuromyelitis optica (NMO) and spinocerebellar ataxia (SCA), among other neurodegenerative diseases, may also be used in the treatment of stroke. In addition, this new class of Nrf2 activators could also be used to treat autoimmune diseases, diabetes and kidney disease, among other chronic diseases. The present invention also relates to processes for the preparation of such compounds. Background technique [0002] Neurodegenerative diseases are incurable diseases that cause progressive dege...
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Application Information
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