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Tetramethylpyrazine ferulate crystals for suppressing platelet aggregation and thrombosis and preparation method thereof

A technology of platelet aggregation and ferulic acid, which is applied in blood diseases, pharmaceutical formulations, organic active ingredients, etc., can solve the problem of not being able to provide a single pure crystal of ligustrazine ferulic acid, and achieve the effect of product toxicity and adverse reaction control

Inactive Publication Date: 2011-05-18
GUANGDONG PHARMA UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] The purpose of the present invention is to overcome the deficiency that the prior art cannot provide a single pure crystal of ligustrazine ferulic acid, and provide a monoclinic crystal of ligustrazine ferulic acid that inhibits platelet aggregation and resists thrombus formation

Method used

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  • Tetramethylpyrazine ferulate crystals for suppressing platelet aggregation and thrombosis and preparation method thereof
  • Tetramethylpyrazine ferulate crystals for suppressing platelet aggregation and thrombosis and preparation method thereof
  • Tetramethylpyrazine ferulate crystals for suppressing platelet aggregation and thrombosis and preparation method thereof

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Experimental program
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Embodiment Construction

[0019] Mix Ligustrazine (tetramethylpyrazine) 2.8g and acetone 45mL, heat and stir to dissolve, then add ferulic acid 4.0g, reflux at 333K for 1 hour, filter and dry the reaction mixture after staying in the container for 5 days, and obtain the present invention Crystals, yellow crystals. Dissolve the yellow crystals in 45 mL of acetone, filter, vacuum-dry to half the volume of the filtrate, place on a clean crystallization bench, crystallize at room temperature, and crystallize for 6 hours to obtain ligustrazine ferulic acid monoclinic crystals. The crystal structure is monoclinic, and the space group is P2 1 / n, the cell parameters are: α=90°, β=93.654(6)°, γ=90°, the unit cell volume is

[0020] The following are the measured parameters of the crystal:

[0021] Instrument: X-ray crystal diffractometer Nova diffactometer Cu target: Nova X-ray source mirror

[0022] Scanning diffraction angle: unit cell 3.6-71.3°; atomic position 3.6-68.3°

[0023] Data processing...

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Abstract

The invention discloses tetramethylpyrazine ferulate crystals for suppressing platelet aggregation and thrombosis. The crystals are of a monoclinic system, wherein a space group is P21 / n; and the unit cell parameters are that: alpha is equal to 90 degrees, beta is equal to 93.654(6) degrees, gamma is equal to 90 degrees, unit cell volume is 1327.70(16) angstrom<3>, and a dihedral angle between a pyrazine ring and a benzene ring is 69.43(11) degrees. The invention also discloses a preparation method of the tetramethylpyrazine ferulate crystals, which comprises the following steps of: mixing tetramethylpyrazine and acetone; heating, stirring and dissolving; adding ferulic acid; performing 333K refluxing; retaining reaction mixture in a container for multiple days and then filtering and drying to obtain yellow crystals; dissolving the yellow crystals in 45mL of acetone; filtering; drying under vacuum until the volume is half of that of filtrate; and crystallizing on a clean crystallizingtable to prepare the tetramethylpyrazine ferulate crystals.

Description

technical field [0001] The invention relates to the field of compound crystals, in particular to a ligustrazine ferulic acid crystal that inhibits platelet aggregation and resists thrombus formation. Background technique [0002] Chinese patent 00114239.9 (authorized notification number 1173958C) discloses a compound ligustrazine ferulic acid, which inhibits platelet aggregation and antithrombosis, and its preparation method and application. The structural formula of this compound is as follows: [0003] [0004] The compound can significantly inhibit the platelet aggregation induced by ADP, collagen and thrombin, and has a depolymerization effect on the aggregated platelets, has an obvious inhibitory effect on thrombus formation, and can dissolve the formed thrombus. The compound also has analgesic properties. The compound can be used to prepare platelet aggregation inhibitors, antithrombotic drugs, thrombolytic drugs, stroke drugs, migraine drugs and the like. In the...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D241/12A61K31/4965A61P7/02A61P25/06
Inventor 谭载友朱尔佳罗琳林卓辉颜锐思
Owner GUANGDONG PHARMA UNIV