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Carboxylic acid derivative compound and preparation method and application thereof

A compound and pharmaceutical technology, applied in the field of novel carboxylic acid derivative compounds, can solve the problems of elevated transaminase, creatine kinase, and liver function damage in patients, and achieve lower cholesterol and low-density lipoprotein with low toxicity Effect

Active Publication Date: 2013-05-08
SHANGHAI SHYNDEC PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, long-term use of statins will not only cause digestive system symptoms such as upper abdominal discomfort, but also liver function damage, elevated transaminases, muscle pain, and elevated creatine kinase in a considerable number of patients.

Method used

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  • Carboxylic acid derivative compound and preparation method and application thereof
  • Carboxylic acid derivative compound and preparation method and application thereof
  • Carboxylic acid derivative compound and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0079] Embodiment 1: the preparation of compound 1

[0080] 1 g of bezafibrate, 0.74 g of dicyclohexylcarbodiimide, 0.52 g of 1-Boc piperazine, and 60 ml of dichloromethane were placed in a 100 ml single-necked bottle, reacted at room temperature for 4 hours, evaporated to dryness, and recrystallized from ethanol to obtain Put 1.22g of white solid into a 50ml single-necked bottle, add 20ml of dichloromethane and 4ml of trifluoroacetic acid, stir for 1 hour, adjust the pH of the system to alkaline with 1mol / L potassium carbonate aqueous solution, dry the organic layer, concentrate, and recrystallize from ethanol. Obtain 0.7g of white solid, put it into a 50ml single-necked bottle, 30ml of tetrahydrofuran, 0.35g of 2-amino-1-(4-hydroxyphenyl)ethanone, 0.5g of potassium carbonate, monitor the end point of the reaction by TLC, and obtain the target by column chromatography Compound 790mg. MS (ESI): 564 (M+H + ).

Embodiment 2-6

[0081] Embodiment 2-6: the preparation of compound 2-compound 6

[0082] Using the raw materials corresponding to the target compound 2-6, the operation method of Example 1 was used to prepare. The specific steps are omitted here.

Embodiment 7

[0083] Embodiment 7: the preparation of compound 7

[0084] 1g of butyryl chloride, 0.71g of 2-amino-1-(4-hydroxyphenyl)ethanone, 2.1g of triethylamine, and 60ml of dichloromethane were placed in a 100ml single-necked bottle, reacted at room temperature for 4 hours, and evaporated to dryness. Column chromatography obtained 2.63 g of the target compound. MS (ESI): 292 (M+H + ).

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Abstract

The invention provides a carboxylic acid derivative compound. The compound as shown in the formula (I) or the pharmaceutically acceptable salt thereof provided by the invention not only can reduce the level of triglyceride in high fat model animal blood, but also has the good function of reducing cholesterol and low-density lipoprotein and the effects of promoting biliation, reducing content of cholesterol in bile and increasing the content of bile acid, and also has the effect of preventing and treating gallstone when being applied to a golden gopher gallstone model. The particular importance is that the compound or the pharmaceutically acceptable salt thereof provided by the invention is low in toxicity.

Description

technical field [0001] The present invention relates to a class of novel carboxylic acid derivative compounds, their preparation method and application. Specifically, a new carboxylic acid derivative compound composed of a suitable raw material (such as an amine compound or a halogenated compound) and a carboxylic acid compound and its preparation method and application are selected. 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 researc...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D295/185C07C233/31C07C231/12C07C69/16C07C67/11C07C235/10C07C309/73C07C303/28C07C323/32C07C319/20C07C233/73C07C69/708C07C327/28A61K31/495A61K31/222A61K31/165A61K31/255A61K31/235A61K31/216A61K31/265A61P3/06A61P1/16
Inventor 于振鹏王国平
Owner SHANGHAI SHYNDEC PHARMA CO LTD
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