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Flavonol derivative and use for anti-platelet aggregation

A technology of anti-platelet aggregation and hydroxyflavone, which is applied in the field of medicine, can solve problems such as toxic side effects, insufficient stability, and inaccurate curative effect, and achieve the effect of simple synthesis method

Inactive Publication Date: 2014-03-12
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Due to many factors affecting platelet aggregation, some drugs still have shortcomings such as inaccurate curative effect, insufficient stability, and toxic and side effects. Strong, broad-spectrum platelet aggregation inhibitors that can inhibit a variety of inducers are still the current research direction

Method used

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  • Flavonol derivative and use for anti-platelet aggregation
  • Flavonol derivative and use for anti-platelet aggregation
  • Flavonol derivative and use for anti-platelet aggregation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] Example 1: 2'-fluoro-7-hydroxyflavone

[0024] Put 0.03mol 2',4'-dihydroxyacetophenone, 0.22mol anhydrous potassium carbonate, and 150mL dry acetone into a 250mL round bottom flask, and slowly add 0.06mol o-fluorobenzoyl chloride dropwise at room temperature. After dropping, it was heated to reflux for 12 hours. Cool, filter with suction, and wash the filter cake with a small amount of acetone. The filter cake was acidified to pH 4-5 with dilute hydrochloric acid, suction filtered, washed and dried. Recrystallization was done with acetone. Add 0.022mol of 1-[2-hydroxyl-4-(2-fluorobenzoyloxy)phenyl]-3-(2-fluorophenyl)]-1,3-propanedione to 100mL cone after recrystallization Add 36mL of concentrated sulfuric acid to a flask, place in an ice bath, and stir for 4 hours. The reaction was stopped, and the reaction solution was poured into a large amount of ice water, and a pale white solid was precipitated. After suction filtration, the filter cake was added to 150 mL of ...

Embodiment 2

[0025] Example 2: 2'-methyl-7-hydroxyflavone

[0026] According to the method for embodiment 1, by 2 ', 4'-dihydroxyacetophenone, o-toluyl chloride reaction obtains white solid. Yield: 38.4%. MS m / z (M): 252.26. 1 H-NMR (DMSO), δ (ppm): 2.54 (3H, s), 6.62 (1H, s), 6.89 (1H, s), 7.44 (2H, m), 7.67 (2H, m), 7.92 (2H , m), 10.92 (1H, s).

Embodiment 3

[0027] Example 3: 2'-chloro-7-hydroxyflavone

[0028] According to the method for embodiment 1, by 2', 4'-dihydroxyacetophenone, o-chlorobenzoyl chloride reaction obtains white solid. Yield: 27.6%. MS m / z (M): 272.68. 1 H-NMR (DMSO), δ (ppm): 6.49 (1H, s), 6.88 (1H, s), 6.89-6.98 (1H, m), 7.51-7.69 (4H, m), 7.76-7.79 (1H, d), 10.94 (1H, s).

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Abstract

The invention belongs to the technical field of medicine, and relates to hydroxy flavone derivatives and application of platelet aggregation resistance thereof. A structural general formula of the hydroxy flavone derivatives is shown as follow; and acid addition salts applicable to the hydroxy flavone derivatives and analogs thereof pharmaceutically can be used as the platelet aggregation inhibitor. In a structural formula I and a structural formula II, R1, R2, R3, R4 and R5 are the same or different, and can be H, halogen, OH, CF3, NO2, NH2, CH3 and OCH3; and R' and R'' are the same or different, and can be the H, the halogen, CH2OH, COOH and CH2Cl. The method for synthesizing compounds is prepared by Baker Venkataraman recomposition and concentrated sulfuric acid cyclization and other methods. The method for synthesizing the compounds is simple, is applicable to industrial production, and is steadier than natural analogs. A biological activity assay shows that the compounds have activities of analgesis, anti-inflammation and anticoagulation, and are the platelet aggregation inhibitor.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to a hydroxyflavone derivative and its anti-platelet aggregation application. Background technique [0002] Clinical studies have shown that common cardiovascular and cerebrovascular diseases such as hypertension, diabetes, angina pectoris, myocardial infarction, cerebral infarction and cerebral hemorrhage are all related to changes in platelet function and abnormal blood rheology (Tianjin Medicine, 1992, 20 (11):684). Therefore, preventing platelet aggregation is of great significance. [0003] Platelets are produced by the lysis of mature megakaryocytes in the bone marrow. The newly formed platelets are large in size, have the ability to synthesize proteins, have strong adhesion, are easy to aggregate and release reactions, and have hemostatic function. At present, it is believed that the physiological activities of platelets mainly include three aspects: adhesion, aggregation an...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D311/30A61K31/352A61P7/02
Inventor 胡春洪秀云刘晓平黄二芳宋爱华刘洋王世辉
Owner SHENYANG PHARMA UNIVERSITY