Applications of emodin succinyl ester compound in preparing lipid-lowering medicines

A technology of emodin succinyl ester and emodin succinyl ethyl ester, which is applied in the field of medicine, can solve the problems of liver tissue cell biochemical changes, cardiac rhabdomyolysis, and restriction of long-term medication, and achieve safe and effective hyperlipidemia, oral administration Absorption, the effect that facilitates the absorption of organisms

Active Publication Date: 2018-06-22
JIANGSU KANION PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, long-term or high-dose use of statins may cause serious adverse reactions such as changes in the biochemistry of liver tissue cells or cardiac rhabdomyolysis, which limits their long-term use.

Method used

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  • Applications of emodin succinyl ester compound in preparing lipid-lowering medicines
  • Applications of emodin succinyl ester compound in preparing lipid-lowering medicines
  • Applications of emodin succinyl ester compound in preparing lipid-lowering medicines

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0054] The preparation of embodiment 1 emodin ethyl succinate

[0055] Take succinic anhydride (1.0g, 10mmol) and place it in a 10mL round-bottomed flask, use ethanol (3.5mL, 60mmol) as a solvent, heat and reflux for 4 hours, and distill off excess ethanol under reduced pressure to obtain a light yellow oil, namely succinic acid mono Ethyl ester (1.4 g, 96%), this product was carried on to the next reaction without isolation.

[0056] Get monoethyl succinate (1.0g, 6.8mmol) and place in a 10mL round-bottomed flask, use thionyl chloride (4.0g, 34.0mmol) as solvent, heat to reflux for 2 hours, and remove excess oxychloride by distillation under reduced pressure. The sulfone was obtained as a light yellow oily product, namely ethyl succinic acid chloride (1.1 g, 98%), and the product was directly carried on to the next reaction without separation.

[0057] Take emodin (1.0g, 3.7mmol) and pyridine (0.45g, 5.6mmol) in a 10mL round-bottomed flask, use dichloromethane (3mL) as solve...

Embodiment 2

[0062] The preparation of embodiment 2 emodin ethyl succinate

[0063] Take succinic anhydride (10g, 100mmol) and place it in a 150mL round-bottomed flask, use ethanol (40mL, 600mmol) as a solvent, heat and reflux for 6 hours, and distill off excess ethanol under reduced pressure to obtain a light yellow oil that is monoethyl succinate (14 g, 96%), the product was directly carried on to the next reaction without isolation.

[0064] Get monoethyl succinate (10g, 68mmol) and place in a 150mL round-bottomed flask, use thionyl chloride (40g, 340mmol) as a solvent, heat and reflux for 2 hours, and remove excess thionyl chloride by distillation under reduced pressure to obtain light The yellow oil was succinic acid monoethyl chloride (11 g, 98%), and the product was directly carried on to the next reaction without isolation.

[0065] Get emodin (10g, 37mmol) and triethylamine (2.3g, 22mmol) and place in a 250mL round-bottomed flask, use dichloromethane (3mL) as solvent, slowly drop...

Embodiment 3

[0068] The preparation of embodiment 3 emodin ethyl succinate

[0069] Take succinic anhydride (10g, 100mmol) and place it in a 150mL round-bottomed flask, use ethanol (20mL, 434mmol) as a solvent, heat and reflux for 2 hours, and distill off excess ethanol under reduced pressure to obtain a light yellow oil that is monoethyl succinate (14 g, 96%), the product was directly carried on to the next reaction without isolation.

[0070] Get monoethyl succinate (10g, 68mmol) and place in a 150mL round-bottomed flask, use thionyl chloride (20g, 170mmol) as a solvent, heat and reflux for 1 hour, and remove excess thionyl chloride by distillation under reduced pressure to obtain light The yellow oil was succinic acid monoethyl chloride (8 g, 98%), and the product was directly carried on to the next reaction without isolation.

[0071] Take emodin (10g, 37mmol) and ammonia water (1.5g, 44mmol) and place in a 250mL round-bottomed flask, use dichloromethane (3mL) as solvent, slowly add s...

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Abstract

The invention discloses applications of an emodin succinyl ester compound in preparing lipid-lowering medicines, belonging to the technical field of medicines. The emodin succinyl ester compound has the structure (R is C1-5 alkyls) as shown in the formula I. The pharmacological experiment is carried out on the experiment mixed type rats with hyperlipemia, and the result proves that the emodin succinyl ester compound provided by the invention is superior to emodin, and has the advantages that the lipid-lowering effect is obvious, the safety is good, the medication is simple and convenient, theraw materials are cheap and easily available, and the transportation and storage are convenient. The emodin succinyl ester compound provided by the invention has the wide application prospect in the field of preparation of the lipid-lowering medicines.

Description

technical field [0001] The invention relates to a new blood lipid-lowering compound emodin succinyl ester compound and its application. It belongs to the field of medical technology. Background technique [0002] With the improvement of living standards, people's dietary structure has changed, and the intake of cholesterol and saturated fatty acids has increased significantly, while the amount of exercise is relatively insufficient, resulting in an increase in the incidence of hyperlipidemia year by year. Hyperlipidemia refers to excessive blood lipid levels, such as the increase of total cholesterol (total cholesterol, TC), triglyceride (triglyceride, TG) and low density lipoprotein (low density lipoprotein, LDL-C) in serum, And the reduction of high-density lipoprotein (high density lipoprotein, HDL-C), can directly cause some diseases that seriously endanger human health, such as atherosclerosis, coronary heart disease and so on. Hyperlipidemia can also lead to fatty li...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/222A61P3/06C07C69/40C07C67/14
CPCA61K31/222C07C69/40
Inventor 杨宝峰许超千王金辉李欣
Owner JIANGSU KANION PHARMA CO LTD
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