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Novel compound as well as preparation method and application thereof

A technology of compounds and mixtures, applied in organic chemistry, drug combination, nervous system diseases, etc., can solve problems such as limitations

Active Publication Date: 2021-10-29
NANTONG UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Dopamine-producing cells in the brain gradually lose their ability to affect the nervous system, limiting the patient's ability to control their muscles

Method used

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  • Novel compound as well as preparation method and application thereof
  • Novel compound as well as preparation method and application thereof
  • Novel compound as well as preparation method and application thereof

Examples

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Embodiment Construction

[0019] 1. N-((4-hydroxycarbamoyl)benzyl)-1-(3,4,5-trimethoxyphenyl)-9H-pyrido[3,4-b]indole-3- Preparation and purity identification of carboxamide

[0020] N-((4-Hydroxycarbamoyl)benzyl)-1-(3,4,5-trimethoxyphenyl)-9H-pyrido[3,4-b]indole-3-carboxamide The preparation process steps are as follows: Dissolve L-tryptophan (5g, 24.5mmol) in acetic acid (50mL), heat to 90°C and stir for 20min, then add 3,4,5-methoxy-benzaldehyde (4.9g, 25.0 mmol) for 6h. After the reaction was finished, the pH was adjusted to neutral with 2M NaOH, and filtered by suction to obtain Compound 3 as a white solid.

[0021] Compound 3 (5g, 13.2mmol) was dissolved in DMF (10ml), cooled in ice, potassium permanganate (4.172g, 26.4mmol) was added, and reacted at room temperature for 1 hour. After the reaction was finished, filter with suction, add the remaining solution into water, and filter with suction to obtain compound 4.

[0022] Compound 4 (0.45g, 1.2mM), EDCI (0.27g, 1.44mM), DMAP (17mg, 0.14mM), ...

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Abstract

The invention discloses a novel compound as well as a preparation method and application thereof, the chemical structural formula of the novel compound is shown in the specification, and the invention provides application of N-((4-hydroxycarbamyl) benzyl)-1-(3, 4, 5-trimethoxyphenyl)-9H-pyrido [3, 4-b] indole-3-carboxamide in preparation of a medicine for treating Parkinson's disease. The effect is excellent and the preparation is simple.

Description

technical field [0001] The present invention relates to a kind of N-((4-hydroxycarbamoyl)benzyl)-1-(3,4,5-trimethoxyphenyl)-9H-pyrido[3,4-b]indole -3-Carboxamide and its preparation method and use. Background technique [0002] Parkinson's disease (PD), also known as Parkinson's disease, is the second largest neurodegenerative disease after Alzheimer's disease and seriously affects the quality of human life. According to statistics, one out of every 800 people in the world suffers from Parkinson's disease. By 2030, due to the acceleration of the aging process, the prevalence rate of Parkinson's disease will double, and it is estimated that there will be more than 9 million patients. The direct medical costs of the patients are estimated to be over US$10,000 per year, placing a heavy burden on families and society. Parkinson's disease is characterized by progressive, multiple, and insidious onset. The main manifestations are slowness of movement, muscle rigidity, resting tr...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D471/04A61P25/16
CPCC07D471/04A61P25/16
Inventor 孙诚凌勇李冰
Owner NANTONG UNIVERSITY