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Benzofuran compounds and their medicinal uses

A technology for benzofuran and compound, which is applied in the field of benzofuran compounds and their medicinal uses, can solve problems such as difficulty in controlling intestinal symptoms, and achieve the effects of inhibiting fat absorption, preventing catalytic decomposition, and being highly selective.

Inactive Publication Date: 2015-12-02
SHENYANG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, Xenical is the best-selling pancreatic lipase inhibitor in the market, which has the characteristics of strong activity and good stability, but it also has the disadvantages of difficult-to-control intestinal symptoms, greasy stools, vomiting and abdominal distension.

Method used

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  • Benzofuran compounds and their medicinal uses
  • Benzofuran compounds and their medicinal uses
  • Benzofuran compounds and their medicinal uses

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0056] Example 1: Preparation of 4-[2-(benzofuran-7 base)ethoxy]benzamide (Compound No. 01)

[0057] 1. Preparation of 7-(2-bromoethyl)benzofuran

[0058]Add 18.00g (0.13mol) of 7-hydroxybenzofuran, 22.68g (0.14mol) of 1,2-dibromoethane, 6.00g (0.04mol) of potassium iodide, and 49.63g (0.36mol) of potassium carbonate into the reaction flask. Acetone was used as solvent and heated to reflux for 3.5h. Suction filtration, rotary evaporation to remove acetone, add an appropriate amount of petroleum ether to dissolve, extract once with 5% NaOH aqueous solution, collect the organic layer and dry it with anhydrous magnesium sulfate. Filtrate, and remove petroleum ether by rotary evaporation to obtain a light yellow oil, add a small amount of petroleum ether to freeze, and a white solid precipitates out. Filter and dry to obtain 22.36g of white solid, yield 69.13%, mp: 72.7-74.5°C. GC-MS m / z: 239.9; 1 H-NMR (CDCl 3 )δ(ppm): 1.98(2H,m), 2.20(2H,m), 2.71(2H,t), 3.72(2H,t), 4.06(2H,...

Embodiment 2

[0065] Example 2: Preparation of N,N-dimethyl-4-[2-(benzofuran-7yl)ethoxy]benzamide (Compound No. 02)

[0066] According to the method of example 1, by 4-[3-(chroman-7-oxygen) propoxyl group] benzoic acid 0.66g (0.002mol), dimethylamine 0.09g (0.002mol), EDC0.42g (0.0022 mol), HOBt0.03g (0.0002mol), triethylamine 1.00g (0.01mol) to give 0.51g of white solid, yield 78.46%, mp: 118.4-119.2℃. LC-MS m / z: 326.1 ([M+H] + ),348.1([M+Na] + ),364.1([M+K] + ); 1 H-NMR (CDCl 3 )δ (ppm): 3.10 (6H, s), 4.28 (2H, m), 4.32 (2H, m), 6.52 (2H, d, J =8.4Hz),6.82(2H,d, J =7.5Hzt),6.98(2H,d, J =8.7Hz),7.08(2H,m),7.20(1H,d, J =7.8Hz),7.45(1H,d, J =8.4Hz),7.66(2H,d, J =8.7Hz); IR(KBr)υ / cm -1 : 3318, 2719, 1642, 1153, 1046, 1153, 1122, 1008, 831, 612.

Embodiment 3

[0067] Example 3: Preparation of N,N-diethyl-4-[2-(benzofuran-7yl)ethoxy]benzamide (Compound No. 03)

[0068] According to the method of example 1, by 4-[3-(chroman-7-oxygen) propoxyl group] benzoic acid 0.66g (0.002mol), diethylamine 0.15g (0.002mol), EDC0.42g (0.0022 mol), HOBt0.03g (0.0002mol), triethylamine 1.00g (0.01mol) to give 0.53g of white solid, yield 74.65%, mp: 129.3-131.2℃. LC-MS m / z: 354.2 ([M+H] + ),376.1([M+Na] + ),392.2([M+K] + ); 1 H-NMR (CDCl 3 )δ(ppm): 1.02(6H,t, J =2.4Hz),2.98(4H,q, J =2.4Hz),4.27(2H,m),4.34(2H,m),6.54(2H,d, J =8.4Hz),6.85(2H,d, J =7.5Hzt),7.02(2H,d, J =8.7Hz),7.12(2H,m),7.21(1H,d, J =7.8Hz),7.55(1H,d, J =8.4Hz),7.69(2H,d, J =8.7Hz); IR(KBr)υ / cm -1 : 3326, 2765, 1621, 1415, 1354, 1115, 1098, 1096, 1060, 732.

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Abstract

The invention discloses a benzofuran compound and a medical application thereof, and relates to a compound and an application thereof. A general formula of the compound is as shown in the specification, wherein R and R' are independently selected from hydrogen, methyl, ethyl or tertiary butyl; or the R and R', together with nitrogen atoms connected to the R and R', form pyrrolidyl, piperidyl or morpholinyl. The compound, disclosed by the invention, through an enzyme inhibiting property efficacy and other biochemical parameters thereof, can achieve an effective treatment effect by an expected usable dosage range which is about 0.01-10mg / kg per day; the compound is bound or embedded in a soluble and / or biodegradable polymer and is coated on a Stent's impression material; such polymer contains polyvinylpyrrolidone, polyhydroxy-propyl isobutylene amide-phenol, and a cross-linked or amphiphilic block copolymer of hydrogel.

Description

technical field [0001] The present invention relates to a compound and its use, in particular to a benzofuran compound and its medical use. Background technique [0002] Obesity is a common disease worldwide. In recent years, the incidence of obesity has been increasing all over the world, especially in developed countries. Due to the rapid development of the economy and the continuous improvement of living standards, the problems of insufficient exercise and relative excess energy intake have always existed in the lifestyle of modern people, which has led to the energy intake of many modern people exceeding energy consumption, and the excess energy Part of it will be stored as fat in adipose tissue, leading to obesity, and obesity can cause a variety of metabolic abnormalities, which is one of the main risk factors for diabetes and cardiovascular diseases, and is associated with increased morbidity and mortality of cardiovascular diseases . At present, traditional non-dru...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D307/79A61K31/343A61K31/5377A61K31/4525A61K31/4025A61P3/04A61K49/00
CPCC07D307/79
Inventor 谭日红
Owner SHENYANG UNIV
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