Furocoumarin compound with hypertension activity reducing function and preparation method thereof

A technology of furanocoumarins and compounds, which is applied in the field of biomedicine, can solve the problems of toxic and side effects of chemical drugs, and the unforeseen effects of chemical drug treatment, and achieve the effects of cheap and easy-to-obtain reagents, mild reaction conditions, and simple operation

Inactive Publication Date: 2010-10-13
XI AN JIAOTONG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, due to the different degrees of toxic and side effects of chemical drugs themselves, hypertension drugs with different mechanisms of action have different shortcomings, which often make the chemical drug treatment of hypertension fail to achieve the desired effect; and enhance the long-term effect of antihypertensive drugs Sex and stationarity are effective ways to improve the effect of antihypertensive drugs

Method used

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  • Furocoumarin compound with hypertension activity reducing function and preparation method thereof
  • Furocoumarin compound with hypertension activity reducing function and preparation method thereof
  • Furocoumarin compound with hypertension activity reducing function and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] Example 1 In the structural formula, n is 2 and forms a double bond, and R is a compound of dimethyl, prepared by the following steps:

[0039] 1) Xanthotoxin (1) is demethylated by boron tribromide to obtain the compound Xanthoxylin (2)

[0040] Take 4.32g (20.00mmol) prickly ash toxin in a 250ml eggplant-shaped bottle, add 73ml of anhydrous dichloromethane, shake well to dissolve, put it in an ice bath under nitrogen protection, and stir for 10-15min; at the same time, put Dissolve 6.88ml of boron tribromide in 73ml of anhydrous dichloromethane to prepare a 1mol / L boron tribromide-dichloromethane solution for use.

[0041] When the temperature inside the eggplant-shaped bottle is constant, place the prepared boron tribromide-dichloromethane solution in a constant pressure dropping funnel, slowly drop it into the eggplant-shaped bottle stirred in an ice bath, and finish the dripping within 30 minutes. After the drop, the ice bath was removed, and the reaction was carr...

Embodiment 2

[0049] Example 2 The compound in which n is 2 and R is dimethyl in the structural formula is prepared by the following steps:

[0050] Step 1) is the same as in Example 1, that is, the preparation steps from the compound xanthotoxin (1) to the compound xanthoxylin (2) are the same; after that, the etherification reaction between the phenolic hydroxyl group and isopentyl bromide occurs, specifically:

[0051] Dissolve 0.40g (2.00mmol) of compound (2) in 10ml of treated anhydrous N,N-dimethylformamide (DMF), add 0.83g (6.00mmol) of anhydrous potassium carbonate, stir at room temperature for 30min, and then Add 0.37ml (3.00mmol) of isopentyl bromide, and react in an oil bath at 80°C for 20 hours under nitrogen protection. After the reaction was cooled to room temperature, the whole system was poured into ice water, stood still until the ice melted, extracted several times with ethyl acetate until the ethyl acetate layer was colorless, and after TLC showed that there was no produc...

Embodiment 3

[0055] Example 3 In the structural formula, n is 2 and forms a double bond, and R is a compound of a hydrogen atom, which is prepared by the following steps:

[0056] Step 1) is the same as in Example 1, that is, the preparation steps from the compound xanthotoxin (1) to the compound xanthoxylin (2) are the same; after that, the etherification reaction between the phenolic hydroxyl group and allyl bromide occurs, specifically:

[0057] Dissolve 0.40g (2.00mmol) of compound (2) in 10ml of treated anhydrous N,N-dimethylformamide (DMF), add 0.83g (6.00mmol) of anhydrous potassium carbonate, stir at room temperature for 30min, and then Add 0.25 ml (3.00 mol) of allyl bromide, and react in an oil bath at 80° C. for 19 hours under nitrogen protection. After the reaction was cooled to room temperature, the whole system was poured into ice water, and stood still until the ice melted, and light brown crystals precipitated, filtered with suction, washed with a small amount of water seve...

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Abstract

The invention discloses a furocoumarin compound with a hypertension activity reducing function and preparation method thereof; the furocoumarin compound has similar nature to imperatorin, shows the activity of dilating blood vessels in isolated vascular ring tension research, and can be applied to the preparation of antihypertensive drugs. The preparation method of the furocoumarin compound has the advantages of easily available raw material sources, mild reaction conditions, simple reaction process operation, and inexpensive and easily available reagent.

Description

technical field [0001] The invention relates to the technical field of biomedicine, and relates to a compound for lowering blood pressure, in particular to a furanocoumarin compound with blood pressure lowering activity and a preparation method thereof. Background technique [0002] Hypertension is currently one of the major diseases that seriously affect human health and threaten human life. It is the most common cardiovascular disease and is closely related to myocardial infarction, stroke, coronary heart disease, heart failure, and renal failure. Nearly 3 million people die from cardiovascular and cerebrovascular diseases in our country every year, accounting for 51% of the total death causes in our country every year; and 75% of the surviving patients lose their ability to work to varying degrees, and 40% of them are seriously disabled. Cardiovascular disease has become the number one killer of human beings. The key to preventing and treating cardiovascular and cerebrov...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D493/04A61K31/37A61K31/453A61K31/5377A61P9/12A61P9/08
CPCA61K31/37A61K31/5377A61K31/453A61P9/08A61P9/12
Inventor 贺浪冲张杰李娜贺建宇张彦民周楠李西玲王嗣岑贺怀贞卢闻
Owner XI AN JIAOTONG UNIV
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