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Polyglycol modifier for benzoic acid/nitrobenzoic acid and its synthesis process

A technology of nitrobenzoic acid and polyethylene glycol, which is applied in the field of chemical and medicinal chemical synthesis, can solve the problems of high cost, low yield and high cost of monohydroxypolyethylene glycol/niacin modified products, and achieve low cost, The effect of high production efficiency and short reaction time

Inactive Publication Date: 2007-03-21
EAST CHINA NORMAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But the raw material DCC and DMAP in this method are more expensive, and cost is higher; And the productive rate of the monohydroxypolyethylene glycol / nicotinic acid modifier in this method is very low, is 40%~50%

Method used

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  • Polyglycol modifier for benzoic acid/nitrobenzoic acid and its synthesis process
  • Polyglycol modifier for benzoic acid/nitrobenzoic acid and its synthesis process
  • Polyglycol modifier for benzoic acid/nitrobenzoic acid and its synthesis process

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0052] Preparation of the crude product of the polyethylene glycol modification of benzoic acid in the first step

[0053]Polyethylene glycol is used as a raw material, a refined product of benzoic acid-chloroformylate is added, a solvent is added, and triethylamine is added. The solvent is benzene. The amounts of polyethylene glycol, refined product of benzoic acid-chloroformylate, solvent and triethylamine were 10.6g (2.4mmol), 1.4g (10mmol), 30ml and 3.5ml, respectively. The weight ratio of polyethylene glycol, refined product of benzoic acid-chloroformylate, solvent and triethylamine is 1:(0.05~0.16):(2.5~4.5):(0.1~0.2). Under a nitrogen atmosphere and magnetic stirring, reflux in an oil bath at 80° C. for 24 hours to obtain a crude product of polyethylene glycol-modified benzoic acid. The structural formula of the polyethylene glycol modification of benzoic acid is

[0054]

[0055] In the formula, n represents 90;

[0056] Purification of the crude product of poly...

Embodiment 2

[0065] Preparation of the crude product of the polyethylene glycol modification of benzoic acid in the first step

[0066] Polyethylene glycol is used as a raw material, a refined product of benzoic acid-chloroformylate is added, a solvent is added, and triethylamine is added. The solvent is benzene. The amounts of polyethylene glycol, refined product of benzoic acid-chloroformylate, solvent and triethylamine were 5.3g (2.4mmol), 1.4g, 30ml and 3.5ml respectively. The weight ratio of polyethylene glycol, refined product of benzoic acid-chloroformylate, solvent and triethylamine is 1:(0.1~0.3):(5.0~9.0):(0.2~0.4). Under a nitrogen atmosphere and magnetic stirring, reflux in an oil bath at 60° C. for 24 hours to obtain a crude product of benzoic acid modified with polyethylene glycol. The structural formula of the polyethylene glycol modification of benzoic acid is

[0067]

[0068] In the formula, n represents 45;

[0069] Purification of the crude product of polyethylen...

Embodiment 3

[0073] Preparation of the crude product of the polyethylene glycol modification of benzoic acid in the first step

[0074] Polyethylene glycol is used as a raw material, a refined product of benzoic acid-chloroformylate is added, a solvent is added, and triethylamine is added. The solvent is benzene. The amounts of polyethylene glycol, refined product of benzoic acid-chloroformylate, solvent and triethylamine were 14.8g (2.4mmol), 1.4g, 30ml and 3.5ml respectively. The weight ratio of polyethylene glycol, refined product of benzoic acid-chloroformylate, solvent and triethylamine is 1:(0.03~0.11):(1.8~3.2):(0.07~0.14). Under a nitrogen atmosphere and magnetic stirring, reflux in an oil bath at 90° C. for 24 hours to obtain a crude product of polyethylene glycol-modified benzoic acid. The structural formula of the polyethylene glycol modification of benzoic acid is

[0075]

[0076] In the formula, n represents 136;

[0077] Purification of the crude product of polyethyle...

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Abstract

The present invention relates to one kind of medicine intermediate, and is especially polyglycol modified benzoic acid / nitrobenzoic acid and its synthesis process. The synthesis process includes the first step of reaction of polyglycol, benzoic acid / nitrobenzoic acid and chloroformylating material to obtain crude polyglycol modified benzoic acid / nitrobenzoic acid product, and the second step of purifying the crude product to obtain refined white modified benzoic acid powder product or yellow nitrobenzoic acid powder product. The present invention has rich material source, low cost, simple synthesis path, high production efficiency and other advantages, and the polyglycol modified benzoic acid / nitrobenzoic acid has high medicine carrying amount, slow release effect and raised water solubility.

Description

technical field [0001] The polyethylene glycol modification of benzoic acid / nitrobenzoic acid and a synthesis method thereof relate to the technical field of a pharmaceutical intermediate and its synthesis, and belong to the synthesis technology of chemistry and pharmaceutical chemistry. Background of the invention [0002] Benzoic acid / nitrobenzoic acid is a commonly used pharmaceutical intermediate. Many clinically used drugs have similar molecular structures, and these substances are slightly soluble in water. For example, niacin is a clinically meaningful small molecule drug that requires long-term administration and has a short half-life. In order to maintain a certain blood concentration, it must be administered frequently; tract stimulates. In order to solve the above problems, it is necessary to modify such drugs, which are usually very expensive, and other molecular models need to be used to explore the experimental conditions for modi...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C08G65/48C07C205/57A61K47/48A61K47/60
Inventor 庄小璐宋春梅薛海丽
Owner EAST CHINA NORMAL UNIV
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