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A kind of application of psoralen compound

A technology for psoralen and compound, which is applied in the directions of active ingredients of heterocyclic compounds, medical preparations containing active ingredients, drug combinations, etc. Problems such as unclear process

Active Publication Date: 2019-04-05
XINJIANG TECHN INST OF PHYSICS & CHEM CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although Uyghur medicine has a remarkable effect and advantages in treating vitiligo, its material basis research is weak, and its mechanism of action and metabolic process in vivo and in vitro are not clear, which seriously restricts its secondary development

Method used

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  • A kind of application of psoralen compound
  • A kind of application of psoralen compound
  • A kind of application of psoralen compound

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0083] 9-methyl-2H-furo[2,3-h]benzopyran-2-one (compound 1) and 6-methyl-2H-furo[3,2-g]benzopyran-2- Preparation of ketone (compound 7):

[0084] At room temperature, dissolve 0.11g (1mmol) of resorcinol in 20mL of dry sulfuric acid, stir until completely dissolved, then add 0.161g (1.2mmol) of malic acid, raise the temperature to 120°C, stir well, and detect the reaction by TLC After completion, cool to room temperature, pour the reaction solution into ice water, extract with ethyl acetate after standing, dry with anhydrous sodium sulfate, and remove the solvent in vacuum to obtain 0.140 g of 7-hydroxycoumarin;

[0085] 0.81g (5mmol) 7-hydroxycoumarin and 5g potassium carbonate (36mmol) were dissolved in 50mL acetone, and 0.48mL (6mmo) 2-chloroacetone was added, fully stirred, after TLC detection reaction was complete, cooled to room temperature, The reaction solution was filtered and concentrated, and the residue was eluted with a gradient gradient of petroleum ether:ethyl ...

Embodiment 2

[0094] 8,9-Dimethyl-2H-furo[2,3-h]benzopyran-2-one (compound 2) and 6,7-dimethyl-2H-furo[3,2-g]benzene Preparation of pyran-2-one (compound 10):

[0095] At room temperature, dissolve 0.11g (1mmol) of resorcinol in 20mL of dry sulfuric acid, stir until completely dissolved, then add 0.161g (1.2mmol) of malic acid, raise the temperature to 120°C, stir well, and detect the reaction by TLC After completion, cool to room temperature, pour the reaction solution into ice water, extract with ethyl acetate after standing, dry with anhydrous sodium sulfate, and remove the solvent in vacuum to obtain 0.140 g of 7-hydroxycoumarin;

[0096] Dissolve 0.81g (5mmol) of 7-hydroxycoumarin and 5g of potassium carbonate (36mmol) in 50mL of acetone, and add 0.60mL (6mmo) of 2-chlorobutanone, stir well, and after TLC detects that the reaction is complete, cool to room temperature , the reaction solution was filtered and concentrated, and the residue was eluted with petroleum ether at a volume rat...

Embodiment 3

[0105] 8,9,10,11-tetrahydro-2H-benzofuro[2,3-h]benzopyran-2-one (compound 13) and 6,7,8,9-tetrahydro-2H-benzene Preparation of furo[3,2-g]benzopyran-2-one (compound 16):

[0106] At room temperature, dissolve 0.11g (1mmol) of resorcinol in 20mL of dry sulfuric acid, stir until completely dissolved, then add 0.161g (1.2mmol) of malic acid, raise the temperature to 120°C, stir well, and detect the reaction by TLC After completion, cool to room temperature, pour the reaction solution into ice water, extract with ethyl acetate after standing, dry with anhydrous sodium sulfate, and remove the solvent in vacuum to obtain 0.140 g of 7-hydroxycoumarin;

[0107] 0.81g (5mmol) of 7-hydroxycoumarin and 5g of potassium carbonate (36mmol) were dissolved in 50mL of acetone, and 0.70mL (6mmo) of 2-bromocyclohexanone was added, fully stirred, and after TLC detected that the reaction was complete, it was cooled to At room temperature, the reaction liquid was filtered and concentrated, and the...

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Abstract

The invention relates to application of psoralen compounds .The number of psoralen compounds is 1-20, and the influences of the 20 psoralen compounds on the melanin generation amount in mouse B16 cells are inspected with a no-treatment group and 8-methoxypsoralen (8-MOP) as the negative control and the positive control respectively .The result shows that compared with the negative control, all compounds except the compound 14 can promote the generation of melanin in the B16 cells, the promotion effect is 112-263%, and the promotion effects of the compounds 8, 15, 17, 18 and 20 on melanin generation can reach 200% or above; compared with the positive control, the promotion effect of all compounds except the compounds 11 and 14 on melanin generation is better than that of the positive control, and the promotion effect of the compounds 17 and 18 on melanin generation is twice that of the positive control; 19 psoralen compounds except the compound 14 can all be used for clinically preparing medicines for treating leucoderma.

Description

technical field [0001] The invention relates to the use of a psoralen compound, which is screened by cell activity, and 19 compounds can be used in the clinical preparation of medicines for treating vitiligo. Background technique [0002] Vitiligo is a common spontaneous or idiopathic depigmentation skin disease, known as one of the three chronic skin diseases in the world, afflicting more than 50 million patients worldwide. The incidence rate varies from 0.1% to 8% in different regions and races in the world. The prevalence rate of the general population in my country is about 0.56%. About half of the patients develop the disease before the age of 20, and the prevalence rate of males and females is equal. [7] . Vitiligo mainly manifests as white spots on the skin and mucous membranes and gray / white hairs. Western medicine believes that vitiligo is caused by the dysfunction and loss of the tyrosinase system in the melanocytes of the skin and hair follicles. [0003] Psora...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/366A61K31/37C07D493/04A61P17/00
CPCA61K31/366A61K31/37C07D493/04
Inventor 阿吉艾克拜尔·艾萨牛超窦君
Owner XINJIANG TECHN INST OF PHYSICS & CHEM CHINESE ACAD OF SCI
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