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D(+)beta-(3,4-dihydroxyphenyl)-alpha-hydroxypropionyl hydrazide and preparation method, drug composition and application thereof

A technology of dihydroxyphenyl and composition, which is applied in the preparation of hydrazides, drug combinations, and pharmaceutical formulations, and can solve problems such as inconvenient production of pharmaceutical preparations

Inactive Publication Date: 2011-03-30
SHANDONG LUYE PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Chinese patent CN1583710 provides danshensu isopropyl ester and its synthesis method; Chinese patent CN1868998 provides danshensu borneyl ester, its synthesis method and application, both of which are oily ester derivatives, which are not convenient for the production of pharmaceutical preparations

Method used

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  • D(+)beta-(3,4-dihydroxyphenyl)-alpha-hydroxypropionyl hydrazide and preparation method, drug composition and application thereof
  • D(+)beta-(3,4-dihydroxyphenyl)-alpha-hydroxypropionyl hydrazide and preparation method, drug composition and application thereof
  • D(+)beta-(3,4-dihydroxyphenyl)-alpha-hydroxypropionyl hydrazide and preparation method, drug composition and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] Embodiment 1: the preparation of danshensu hydrazide

[0022] Add 1ml (10mmol) of 98% concentrated sulfuric acid dropwise to 4.0g (20mmol) of Danshensu in methanol solution, heat to reflux, stir and react for 4 hours, evaporate methanol under reduced pressure, extract with ethyl acetate / water, and extract with 0.5% sodium bicarbonate The extract was washed with the solution, dried with anhydrous sodium sulfate, filtered, and the ethyl acetate was distilled off under reduced pressure to obtain 2.42 g of oily D(+)β-(3,4-dihydroxyphenyl)-α-hydroxypropyl methyl ester. rate 56.5%.

[0023] To 2.12 g (10 mmol) of Danshensu methyl ester in 20 ml of methanol solution, 3 ml (50 mmol) of hydrazine hydrate was added dropwise, heated to reflux, stirred and reacted for 6 hours, the solvent was evaporated under reduced pressure, and dried to obtain the target compound, 1.9 g of white powder. The yield is 89.6%, the melting point is 162-164°C (the melting point instrument is not corr...

Embodiment 2

[0027] Embodiment 2: Preparation of Danshensu Hydrazide Injection

[0028] D(+)β-(3,4-dihydroxyphenyl)-α-hydroxypropionohydrazide 10g

[0029] Water for injection 1000ml

[0030]

[0031] 1000 pieces

Embodiment 3

[0032] Embodiment 3: Preparation of Danshensu Hydrazide Tablets

[0033] D(+)β-(3,4-dihydroxyphenyl)-α-hydroxypropionohydrazide 50g

[0034] Lactose 70g

[0035] Sodium Carboxymethyl Cellulose 20g

[0036] Talc 5g

[0037] Magnesium Stearate 3g

[0038] Sodium Laurate 2g

[0039]

[0040] 1000 pieces

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Abstract

The invention provides a novel compound D(+)beta-(3,4-dihydroxyphenyl)-alpha-hydroxypropionyl hydrazide and a preparation method, a drug composition and application thereof to preparing drugs for treating or preventing coronary heart diseases, angina or myocardial infarction. The protective effect of the compound on myocardial ischemia injury caused by ligation of coronary artery is obviously superior to that of salvianic acid A.

Description

technical field [0001] The invention provides a novel hydrazide compound, a preparation method, a pharmaceutical composition containing the compound and an application in preparation of medicines for treating or preventing cardiovascular diseases. technical background [0002] Danshensu, whose chemical name is D(+)β-(3,4-dihydroxyphenyl)-α-hydroxypropionic acid, is the main active ingredient of traditional Chinese medicine Danshen. It is oily. It is reported in the literature that Danshensu has obvious protective effect on myocardial ischemia [Zheng Ruoyun, Fang Sanman, Han Baoming, etc. Protective effect of Danshen water extract on chemically induced myocardial ischemia in rats. Journal of Integrated Traditional Chinese and Western Medicine, 1990, 10 (10 ): 609.; Jiang Wende, Chen Yuhua, Wang Yingping, et. .; Tang Lihui, Wang Xiaoming, Liang Dianquan, et al. Protective effect of Danshensu on myocardial ischemia / reperfusion injury in rats. Chinese Journal of Pathophysiolog...

Claims

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Application Information

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IPC IPC(8): C07C243/32C07C241/04A61K31/165A61P9/00A61P9/10
Inventor 高玉白蒋王林孙盛茂侯建
Owner SHANDONG LUYE PHARMA CO LTD