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Ester compound, preparation method and application thereof

A compound and drug technology, applied in the field of ester compounds, its preparation and application, can solve the side effects of rhabdomyolysis syndrome and other problems, achieve the effect of low toxicity, lower cholesterol and low-density lipoprotein

Active Publication Date: 2011-06-15
SHANGHAI INST OF PHARMA IND CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Attempts to combine the two types of drugs have resulted in severe side effects of rhabdomyolysis syndrome in some patients

Method used

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  • Ester compound, preparation method and application thereof
  • Ester compound, preparation method and application thereof
  • Ester compound, preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0085] Preparation of 4-acetylphenyl 2-[4-[2-(4-chlorobenzamido)ethyl]phenoxy]-2-methylpropanoate

[0086] 2-[4-[2-(4-Chlorobenzamido)ethyl]phenoxy]-2-methylpropionic acid 1g, dicyclohexylcarbodiimide 0.57g, p-hydroxyacetophenone 0.38g , 60ml of dichloromethane was placed in a 100ml single-necked bottle, reacted at room temperature for 5 hours, evaporated to dryness, and recrystallized from ethanol to obtain 2-[4-[2-(4-chlorobenzamido)ethyl]phenoxy] - 4-acetylphenyl 2-methylpropionate 800mg. MS (ESI): 480 (M+H + ). 1 H NMR (400MHz, CDCl 3 )δ(ppm): 1.774(6H), 2.607(3H), 2.898-2.934(2H), 2.687-3.736(2H), 6.019(1H), 6.945-6.967(2H), 7.127-7.182(4H), 7.367 -7.389 (2H), 7.610-7.632 (2H), 7.981-8.003 (2H).

Embodiment 2

[0088] Preparation of 4-propionylphenyl 2-[4-[2-(4-chlorobenzamido)ethyl]phenoxy]-2-methylpropanoate

[0089] 2-[4-[2-(4-Chlorobenzamido)ethyl]phenoxy]-2-methylpropionic acid 1g, dicyclohexylcarbodiimide 0.57g, p-hydroxypropiophenone 0.40g, 60ml of dichloromethane was placed in a 100ml single-necked bottle, reacted at room temperature for 5 hours, evaporated to dryness, and recrystallized from ethanol to obtain 2-[4-[2-(4-chlorobenzamido)ethyl]phenoxy]- 4-propionylphenyl 2-methylpropionate 700mg. MS (ESI): 494 (M+H + ).

Embodiment 3

[0091] Preparation of 2-[4-[2-(4-chlorobenzamido)ethyl]phenoxy]-2-methylpropanoic acid 4-butyrylacetylphenyl ester

[0092] 2-[4-[2-(4-Chlorobenzamido)ethyl]phenoxy]-2-methylpropionic acid 1g, dicyclohexylcarbodiimide 0.57g, p-hydroxybutyrophenone 0.38 g, 60ml of dichloromethane was placed in a 100ml single-necked bottle, reacted at room temperature for 5 hours, evaporated to dryness, and recrystallized from ethanol to obtain 2-[4-[2-(4-chlorobenzamido)ethyl]phenoxy ]-4-butyrylphenyl 2-methylpropionate 600 mg. MS (ESI): 508 (M+H + ).

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Abstract

The invention discloses a compound shown as a formula I or pharmaceutically acceptable salt thereof. In the formula I, R1, R2, R3, R4, R5 and n are defined as the specification. The invention also discloses a preparation method for the compound of the formula I, a composition containing the compound and application of the compound. The compound of the formula I is stable in vitro, has good dissolubility in a pharmaceutically applied organic solvent, and has good bioavailability in the body of an animal. Meanwhile, the invention discloses the preparation method for the compound of the formula I and the application of the compound of the formula I in preparation of medicaments for regulating blood fat and preventing and treating biliary calculus.

Description

Technical field: [0001] The present invention relates to a novel ester compound and its preparation method and application. It specifically relates to an ester formed of p-hydroxyacetophenone and its derivatives and phenoxyaromatic acid, a preparation method and application thereof. Background technique: [0002] Cardiovascular and cerebrovascular diseases are currently the most serious disease that endangers human life and health, and are common and frequently-occurring diseases among middle-aged and elderly people. It ranks first in morbidity and mortality in many countries. Atherosclerosis is the basis of many cardiovascular and cerebrovascular diseases. A large number of experimental and clinical data prove that atherosclerosis is closely related to abnormal blood lipid metabolism. Therefore, lipid-regulating drugs have become an important field of current drug research. [0003] Through prospective, random and controlled clinical studies, it has been proved that some...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C233/73C07C69/738C07C69/712C07C231/12C07C67/08C07C67/14C07D295/108A61K31/216A61K31/495A61P3/06A61P1/16
Inventor 张瑱于振鹏秦燕徐智儒于美静肖璘吴学军檀琼刘珉宇孙海燕刘英孙文劼肖旭华闫兆峰刘畅刘全海
Owner SHANGHAI INST OF PHARMA IND CO LTD
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