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A kind of method for preparing motherwort

A technology of leonurine and leonurine, which is applied in the field of preparing leonurine, can solve problems such as difficulty in separation, and achieves the effects of solving difficulty in separation, being easy to control, and easily obtaining raw materials

Inactive Publication Date: 2011-11-30
FUDAN UNIV
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  • Abstract
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AI Technical Summary

Problems solved by technology

Specifically, the method for preparing motherwort of the present invention is characterized in that, during the synthesis process, the preparation of motherwort by the Gabriel amine-forming method is avoided, and the defect of difficult separation is solved.

Method used

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  • A kind of method for preparing motherwort
  • A kind of method for preparing motherwort
  • A kind of method for preparing motherwort

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Experimental program
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Effect test

Embodiment 1

[0029] The following instruments, reagents and solvents were used in this experiment:

[0030] The nuclear magnetic resonance instrument is JEOL JNM.ECP nuclear magnetic resonance spectrometer; the mass spectrometer is Q.TofUltima Global (ion source: ESI, APCI, MAI, DI). All reagents and solvents were of imported or domestic analytical grade, and the solvents were not further processed.

[0031] 1. Synthesis of 4-ethoxycarbonyl-oxygen-syringic acid

[0032]

[0033] In a 1000ml reactor, add 800ml of 1mol / L sodium hydroxide solution, add 66g (0.33mol) of syringic acid under stirring, after dissolving, wait until the temperature of the solution drops below 10°C, add 36.17g of ethyl chloroformate dropwise (0.33mol), control the temperature of the reaction solution at 0-10°C, stir and react for 6 hours, and track the reaction degree with TCL. After the reaction, adjust the pH value to about 6.0 with hydrochloric acid, leave to precipitate white crystals, filter, and obtain a w...

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Abstract

The invention belongs to the field of traditional Chinese medicine pharmacy, and relates to a method for preparing motherurine, comprising: selecting cheap aminobutyric acid as a raw material, through amino group protection and reduction reaction, conveniently synthesizing protected aminobutanol, using benzyl as p-clove The protective group of the acid phenolic hydroxyl group is crystallized after reflux in ethanol-sodium hydroxide aqueous solution, and the benzyl-protected penic acid is synthesized. The benzyl-protected syringic acid is condensed with aminobutanol by using CDI or DCC, and the protected motherwort is in Under the catalytic condition of 10% palladium hydroxide, the motherwort is obtained by hydrogen reduction, and finally the motherwort is synthesized. The method avoids the Gabriel amine-forming method in the prior art to prepare the motherwort, overcomes the separation difficulty, and reduces the use of environment-polluting reagents. The method has the advantages of less separation process, simple operation, mild reaction, easy control, and easy-to-obtain raw materials, and can synthesize the motherwortine in large quantities. The purity of the product is 99.8%, and the structure is consistent with the natural motherwortine.

Description

technical field [0001] The invention belongs to the field of traditional Chinese medicine pharmacy, and relates to a method for preparing motherurine. Background technique [0002] Leonurine is an alkaloid contained in Lamiaceae Leonurus, and there are literature reports on its extraction, separation, pharmacology and structural formula (I) in the prior art. The literature also discloses that motherwortine has the effects of promoting blood circulation and removing stasis, diuresis and swelling, and is a good medicine for gynecology in traditional Chinese medicine. It can inhibit the aggregation of platelets and prevent the formation of thrombus; it can expand peripheral blood vessels and reduce vascular resistance, and has certain antihypertensive and antihypertensive effects. Coronary resistance, and pharmacological effects such as increasing coronary blood flow and protecting the heart. [0003] [0004] According to reports, the content of motherwortine in the raw ma...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C279/08C07C277/08C07C219/14C07C213/02
Inventor 朱依谆魏邦国刘新华潘礼龙刘春华
Owner FUDAN UNIV
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