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Aldehydic acids tetramethylpyrazine ester and method for preparing same

A technology of ligustrazine esters and polyacids, applied in the field of polyacids ligustrazine esters and its preparation, can solve the problems of fast excretion and low bioavailability of ligustrazine

Inactive Publication Date: 2005-12-07
BEIJING INSTITUTE OF TECHNOLOGYGY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] The present invention aims at the problems of rapid excretion and low bioavailability of ligustrazine currently used clinically, and prepares polymer-supported drugs

Method used

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  • Aldehydic acids tetramethylpyrazine ester and method for preparing same

Examples

Experimental program
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Effect test

preparation example 1

[0015] Synthesis of Ligustrazine Polyacrylate from Polyacrylic Acid with Molecular Weight of 800-1000

[0016] (1) Synthesis of 2,5-dimethylol-3,6-dimethylpyrazine (intermediate)

[0017] Dissolve 50.4g of ligustrazine phosphate in 90ml of glacial acetic acid, add 90ml of hydrogen peroxide solution in an oil bath at 98°C, reflux for 24 hours, adjust the pH value to 9-10 with 20% sodium hydroxide solution, and extract with chloroform. Add anhydrous Na 2 SO 4 Drying, filtering, and rotary evaporation can give white Ligustrazine-1,4-bis-nitrogen oxide with a melting point of 212-224°C. Weigh 16.8g ligustrazine-1,4-dinitrogen oxide and dissolve it in 150ml acetic anhydride, reflux for 4h under the condition of oil bath at 150°C, adjust the pH value to 9-10 with 20% sodium hydroxide solution, and let stand 24 hours, extracted with ethyl acetate, added anhydrous Na 2 SO 4 After drying, filtering and rotary evaporation, light yellow 2,5-dimethylol-3,6-dimethylpyrazine can be obt...

preparation example 2

[0023] The steps of Preparation Example 1 were repeated, and polyacrylic acid with a molecular weight of 100,000 was used instead of polyacrylic acid with a molecular weight of 800-1000 to prepare 2,4-dimethylol-3,6-dimethylpyrazine grafted polypropylene ester.

preparation example 3

[0025] Weigh 699.2 mg of 2-hydroxymethyl-3,5,6-trimethylpyrazine to replace 2,5-dimethylol-3,6-dimethylpyrazine, and repeat the steps of Preparation Example 1. Wherein the synthesis of 2-hydroxymethyl-3,5,6-trimethylpyrazine refers to Chinese patent (application number 200310100267X).

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Abstract

The invention provides aldehydic acids tetramethylpyrazine esters, compounds of polyaromatics supported Ligusticum wallichii effective compositions, and the process for their preparation, which comprises converting lateral chains into ligustrazine derivatives of reactive groups, bonding with polyacids under the action of dicyclo hexylcar bodiimide (DCCI), so as to join ligustrazine lateral chains with polymers of functional groups through ester linkages.

Description

technical field [0001] The invention relates to a polymer-supported compound of traditional Chinese medicine active ingredients and a preparation method thereof, relates to the fields of biomedical materials and medicine, and belongs to derivative compounds of ligustrazine. Background technique [0002] Ligustrazine is an alkaloid monomer isolated and purified from Ligusticum chuanxiong, an algae belonging to the genus Umbelliferae. Ligustrazine has a wealth of pharmacological effects. Since the mid-1970s, it has become a commonly used drug for clinical treatment of ischemic cerebrovascular disease in China. However, in the application, it was found that Ligustrazine metabolizes quickly in the body, requires frequent administration, and has obvious peaks and valleys. [0003] In order to solve the above problems, researchers in my country have made some useful attempts, such as chemically modifying Ligustrazine with various small molecules (see "Structure Modification and ...

Claims

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Application Information

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IPC IPC(8): C08F8/14
Inventor 林妮妮王松朱鹤孙
Owner BEIJING INSTITUTE OF TECHNOLOGYGY
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