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Amide compound and preparation method as well as application thereof

一种化合物、选自的技术，应用在有机化合物的制备、亚氨基化合物制备、羧酸酰胺制备等方向，能够解决肌酸激酶升高、病人肝功能损害、转氨酶升高等问题，达到降低胆固醇和低密度脂蛋白的、良好胆固醇和低密度脂蛋白的、毒性低的效果

Active Publication Date: 2012-12-26
SHANGHAI INST OF PHARMA IND CO LTD +1
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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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  • Amide compound and preparation method as well as application thereof
  • Amide compound and preparation method as well as application thereof
  • Amide compound and preparation method as well as application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0091] Embodiment 1: the preparation of compound 01

[0092] 2-(4-(2-(4-chlorobenzamido)ethyl)phenoxy)-2-methylpropionic acid 1g, dicyclohexylcarbodiimide 0.57g, 2-amino-1- 0.5 g of (4-hydroxyphenyl) ethyl ketone and 60 ml of dichloromethane were placed in a 100 ml single-necked bottle, reacted at room temperature for 4 hours, the solvent was evaporated to dryness, and 820 mg of the target compound was obtained by silica gel column chromatography. MS(ESI): 495(M+H + ). 1 H-NMR: 7.720-7.698 (2H, d), 7.629 (1H, s), 7.605-7.584 (2H, d), 7.281 (1H, s), 7.232-7.210 (2H, d), 7.158 (1H, s ), 7.011-6.99 (2H, d), 6.810-6.751 (4H, m), 4.559-4.547 (2H, s), 3.484-3.473 (2H, m), 2.764-2.729 (2H, m), 1.381 (6H , s)

Embodiment 2

[0093] Embodiment 2: the preparation of compound 02

[0094] 2-(4-(2-(4-chlorobenzamido)ethyl)phenoxy)-2-methylpropionic acid 2g, dicyclohexylcarbodiimide 1.2g, 2-amino-1- 0.5 g of (4-hydroxyphenyl)ethanone 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 1.3 g of the target compound was obtained by silica gel column chromatography. MS (ESI): 838 (M+H + ).

Embodiment 3

[0095] Embodiment 3: the preparation of compound 03

[0096] 2-methyl-2-(4-(4-chlorobenzoyl)phenoxy)propionic acid 1g, dicyclohexylcarbodiimide 0.57g, 2-amino-1-(4-hydroxyphenyl) 0.5 g of ethyl ketone and 60 ml of dichloromethane were placed in a 100 ml single-necked bottle, reacted at room temperature for 4 hours, the solvent was evaporated to dryness, and 820 mg of the target compound was obtained by silica gel column chromatography. MS(ESI): 452(M+H + ). 1 H-NMR: 7.8-7.85 (2H, d), 7.7-7.8 (4H, m), 7.6 (1H, m), 7.42-7.53 (2H, d), 7.04-7.13 (2H, d), 6.9-7.1 (2H, d), 6.84 (1H, s), 4.7 (2H, d), 1.65 (6H, s)

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PUM

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Abstract

The invention discloses an amide compound and a preparation method as well as application thereof. The amide compound is specifically a compound shown by a formula I or pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, Q, X and n are defined in the specification. The invention also discloses the preparation method of the compound shown by the formula I, a composition comprising the compound and application of the compound to preparation of medicaments for adjusting blood fat and / or preventing gall stone. The compound shown by the formula I is stable in vitro, has high solubility in pharmaceutically applied organic solvent and has higher bioavailability in animals.

Description

technical field [0001] The present invention relates to a novel amide compound and its preparation method and application. It specifically relates to an amide composed of an amine compound and a carboxylic acid compound, a preparation method and an 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 statins can re...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C235/20C07C231/02C07C251/16C07C249/02C07C325/02A61K31/222A61K31/166A61K31/165A61P3/06A61P1/16
CPCC07C251/16C07C2101/02C07C2101/14C07C231/02A61K31/166C07C249/02C07C325/02A61K31/222C07C251/24C07C235/26A61K31/165C07C235/20C07C235/84C07C2601/02C07C2601/14A61P1/16A61P3/06
Inventor 于振鹏王国平张瑱刘珉宇黄晓玲刘英肖璘蔡立吴学军邓轶方潘绵立陈仁海汤生荣刘全海
Owner SHANGHAI INST OF PHARMA IND CO LTD
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