N-acyl amino glucose and its preparation process

A technology of glucosamine hydrochloride and acyl amino, which is applied in the field of acylation of glucosamine, and can solve problems such as aggravation of diabetes and gout, facial flushing, and ulcer induction

Inactive Publication Date: 2005-06-08
HUNAN UNIV OF SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, niacin requires a large amount of treatment (3-6g / d), and it is easy to produce facial flushing, itching, induced ulcers, and aggravates side effects such as diabetes and gout, which limits its clinical application

Method used

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  • N-acyl amino glucose and its preparation process
  • N-acyl amino glucose and its preparation process
  • N-acyl amino glucose and its preparation process

Examples

Experimental program
Comparison scheme
Effect test

Embodiment

[0019] Take 2-deoxy-2-nicotinamide-β-D-glucose and its preparation method as an example:

[0020] The molecular structural formula of 2-deoxy-2-nicotinamide-β-D-glucose is:

[0021]

[0022] Its whole reaction process is expressed as follows:

[0023]

[0024]

[0025] 1. Synthesis of Nicotinyl Chloride Hydrochloride

[0026] 3-15.0ml SOCl 2 Put it into the reaction flask equipped with HCl gas absorption device, add 0.4∽15g nicotinic acid to it at about -10∽5℃, stir, drop a few drops of anhydrous DMF, and slowly raise the temperature to 60∽85℃ in an oil bath , after reflux for 3h, the excess SOCl was distilled off under reduced pressure 2 , to obtain light yellow powdery solid substance (1) with a yield of 81%.

[0027] 2. Synthesis of 1,3,4,6-tetraoxyacetyl-2-deoxy-β-D-glucosamine hydrochloride

[0028] React quantitative glucosamine hydrochloride in 30∽80mL dilute NaOH solution with 2.5g p-methoxybenzaldehyde for 1∽4h. After filtering, washing and drying, N-p-m...

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Abstract

An N-acylaminoglucose for treating hyperlipemia, hypertriglyceridemia, etc and preventing coronary heart disease, myocardial infarction, and cardiovascular and cerebrovascular diseases is prepared by coupling organic acid with aminoglucose.

Description

technical field [0001] The invention relates to an acylation technology of glucosamine. Background technique [0002] Niacin as a broad-spectrum lipid-regulating drug. It can be used to treat hyperlipidemia, hypertriglyceridemia, low-density lipoprotein (a) hyperlipidemia and hyperproteinemia. Long-term application can reduce the incidence of coronary heart disease, myocardial infarction and other cardiovascular and cerebrovascular diseases. But niacin requires a large amount of treatment (3-6g / d), and it is easy to produce facial flushing, itching, induce ulcers, and aggravate side effects such as diabetes and gout, which limits its clinical application. Contents of the invention [0003] The object of the present invention is N-acyl glucosamine and a process for its preparation. [0004] The object of the present invention is achieved in the following manner: a kind of N-acyl glucosamine, the general structural formula of this compound is: [0005] [0006] where R...

Claims

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Application Information

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IPC IPC(8): C07H5/06
Inventor 郭振楚
Owner HUNAN UNIV OF SCI & TECH
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