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Preparation method and applications of anti-platelet aggregation candidate drug PN531

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

Inactive Publication Date: 2015-08-12
TIANJIN UNIVERSITY OF TECHNOLOGY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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  • Preparation method and applications of anti-platelet aggregation candidate drug PN531
  • Preparation method and applications of anti-platelet aggregation candidate drug PN531
  • Preparation method and applications of anti-platelet aggregation candidate drug PN531

Examples

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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

The invention relates to an anti-platelet aggregation candidate drug PN531 and a preparation method thereof, wherein the molecular formula of PN531 is C23H20O3N2Cl2, and the chemical name of PN531 is 4-methoxy-N,N'-bis(3-chloro-2-methylphenyl)-1,3-benzene diamide. The PN531 preparation steps comprise: 1) adding 3-chloro-2-methylaniline and 4-methoxy-1,3-benzenediacyl chloride to a reaction solvent, uniformly mixing, reacting, and carrying out pressuring reducing distillation to remove the solvent to obtain a compound crude product; and 2) carrying out re-crystallization on the compound crude product by using a re-crystallization solvent to obtain the compound pure product. According to the present invention, the preparation method is simple and is easy to perform; and the prepared PN531 has the strong anti-platelet aggregation activity and establishes the good foundation for further deep research and development of the new anti-platelet aggregation drug and applications thereof.

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 Applications(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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