Preparation method and application of a kind of anti-platelet aggregation candidate drug pn531

An anti-platelet aggregation and drug technology, applied in the preparation of organic compounds, drug combination, carboxylic acid amide preparation, etc., to achieve the effect of simple preparation method and strong anti-platelet aggregation activity

Inactive Publication Date: 2017-12-12
TIANJIN UNIVERSITY OF TECHNOLOGY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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  • Preparation method and application of a kind of anti-platelet aggregation candidate drug pn531
  • Preparation method and application of a kind of anti-platelet aggregation candidate drug pn531
  • Preparation method and application of a kind of anti-platelet aggregation candidate drug pn531

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Experimental program
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Embodiment 1

[0018] A preparation method of anti-platelet aggregation candidate drug PN531, the molecular formula of the anti-platelet aggregation candidate drug of the anti-platelet aggregation candidate drug is C 23 h 20 o 3 N 2 Cl 2 , the compound name is 4-methoxy-N, N'-bis(3-chloro-2-methylphenyl)-1,3-phthalamide, and its chemical structural formula (1) is as follows:

[0019]

[0020] , the reaction solvent is tetrahydrofuran, the recrystallization solvent is methanol, and the preparation steps are as follows:

[0021] 1) Add 1.38g (9.8mmol) of 3-chloro-2-methylaniline and 1.14g (4.9mmol) of 4-methoxy-1,3-phthaloyl chloride into tetrahydrofuran, mix well, and react at 20°C After 72 hours, the solvent was distilled off at 35°C under a pressure of 0.7Mpa to obtain a crude compound;

[0022] 2) The crude compound above was recrystallized with methanol to obtain 1.93 g of the pure compound; yield: 89%. mp: 251-252°C.

Embodiment 2

[0024] A preparation method of an anti-platelet aggregation candidate drug PN531 is basically the same as in Example 1, except that the reaction is carried out at a temperature of 25°C for 48 hours; the reaction solvent is methanol, and the recrystallization solvent is ethyl acetate to obtain the pure compound 1.76 g; Yield: 81%. mp: 251-252°C.

Embodiment 3

[0026] A preparation method of an anti-platelet aggregation candidate drug PN531, which is basically the same as in Example 1, except that the reaction is carried out at a temperature of 45° C. for 30 hours; the reaction solvent is carbon tetrachloride, and the recrystallization solvent is methanol to obtain a pure product of the compound 1.69 g; Yield: 78%. mp: 251-252°C.

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Abstract

An anti-platelet aggregation candidate drug PN531 and a preparation method thereof, the molecular formula of the PN531 is C23H20O3N2Cl2, and the chemical name of PN531 is 4-methoxy-N,N'-bis(3-chloro-2-methylphenyl) -1,3-phthalamide, PN531 preparation steps are as follows: 1) 3-chloro-2-methylaniline and 4-methoxy-1,3-phthaloyl chloride are added in the reaction solvent to mix and react, After the solvent is distilled off under reduced pressure, the crude compound is obtained; 2) the crude compound is recrystallized with a recrystallization solvent to obtain the pure compound. The advantages of the invention are: the preparation method is simple and easy; the prepared PN531 has strong anti-platelet aggregation activity, which lays a good foundation for further in-depth research and development of new anti-platelet aggregation drugs and their applications in the future.

Description

technical field [0001] The invention relates to the preparation of drugs with high anti-platelet aggregation activity, especially the preparation method and application of a candidate anti-platelet aggregation drug PN531. Background technique [0002] Platelet aggregation is a key link in the normal coagulation mechanism, and the adhesion, aggregation and release reactions of platelets lead to thrombus formation. Anti-platelet aggregation drugs refer to drugs that can inhibit the adhesion and aggregation of platelets and inhibit thrombosis, so they play an important role in the treatment of thrombosis. Oral anti-platelet drugs are currently the most commonly prescribed long-term preventive therapy. [0003] In recent years, in order to find newer, more effective and broader-spectrum anti-platelet aggregation drugs, the present invention has made further research on 4-methoxy-1,3-phthalamide compounds. The results of the preliminary screening test for anti-platelet aggregati...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07C235/64C07C231/02A61P7/02
Inventor 刘秀杰李旭孟侠
Owner TIANJIN UNIVERSITY OF TECHNOLOGY
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