Methyl 2-(2-(2,6-dichlorophenylamino)phenyl)acetate and its synthesizing method and application

A technology of dichlorophenylamino and methyl acetate, which is applied in the direction of chemical instruments and methods, medical preparations containing active ingredients, drug combinations, etc., can solve problems such as unusable, high toxicity and side effects, and large damage, and achieve Effect with low toxicity

Inactive Publication Date: 2008-05-28
JILIN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, diclofenac sodium and potassium salt, which are the most clinically used at home and abroad, have strong anti-inflammatory, analgesic and antipyretic effects and are widely used in more than 120 countries and regions in the world, but the toxicity and side effects of these drugs are relatively large, especially The damage to the stomach and liver is relatively large, so that it cannot be used for patients with abnormal gastrointestinal mucosa and abnormal liver function, nor can it be used for children and the elderly

Method used

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  • Methyl 2-(2-(2,6-dichlorophenylamino)phenyl)acetate and its synthesizing method and application
  • Methyl 2-(2-(2,6-dichlorophenylamino)phenyl)acetate and its synthesizing method and application
  • Methyl 2-(2-(2,6-dichlorophenylamino)phenyl)acetate and its synthesizing method and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0049] Get diclofenac potassium (sodium) and dissolve it in water and acidify to obtain 14 g (70%) of diclofenac refined product. (mp is 156-158°C). 21.3g (188.4mmol) of chloroacetyl chloride was added dropwise under ice-cooling, and after the reaction was completed, 12.3g (88.6%) of methyl 2-(2-(2,6-dichlorophenylamino)phenyl)acetate was obtained, as shown below .

[0050]

Embodiment 2

[0052] 2 g (6.8 mmol) of diclofenac and 3.1 ml (76.4 mmol) of anhydrous methanol were sequentially added into the four-necked flask, and heated to reflux for 3 h. Spin-dry to obtain 1.9 g (90.0%) of methyl 2-(2-(2,6-dichlorophenylamino)phenyl)acetate, as shown below.

[0053]

Embodiment 3

[0055] Recipe quantity: 60g of methyl 2-(2-(2,6-dichlorophenylamino)phenyl)acetate, 84g of HPMCE4CR, 60g of anhydrous citric acid, 145.3g of lactose, 0.7g of magnesium stearate, a total of 1000 piece.

[0056] Preparation method: Take 2-(2-(2,6-dichlorophenylamino)phenyl)methyl acetate, HPMCE4CR, anhydrous citric acid, lactose and lubricant, pass through a 100-mesh sieve, mix evenly, and press into tablets In the hopper of the machine, adjust the pressure and filling amount, press into tablets, and get it.

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Abstract

The invention relates to a 2-(2-(2, 6-dichlorophenyl amido) phenyl) methyl acetate, relative synthesis method and application, belonging to the technical field of chemical pharmacy, which comprises that adds acid into diclofenac salt to acidify the salt into diclofenac, reacts diclofenac with methanol, or adds acid into diclofenac salt to acidify the salt into diclofenac, to be reacted with chloracetyl chloride to obtain 2-(2-(2, 6-dichlorophenyl amido) phenyl) methyl acetate. The inventive drug has significant anti-inflammatory and analgesic effects.

Description

technical field [0001] The invention belongs to the technical field of chemical pharmacy and the field of new drug application of compounds. Background technique [0002] Currently, NSAIDs (Nonsteroidal anti-inflammatory drugs, NSAIDs) in the world mainly include the following types according to their chemical structure: [0003] Classification representative drug Salicylates Pyrazolones Carboxylic acid Aromatic acids Phenylacetic acids Indene acetates Naphthalene acetic acid anthraniloids Indoleacetic acids Aryl acids Phenylpropionates heterocyclic aromatic acids Naphthalene Protones Anthranilic acids Oxicams Sulfonanilides Coxibs aspirin, diflunisal Hydroxybuzone, Botasone fenbufen Sulindac Nabumetone Diclofenac Indomethazin, etodolac ibuprofen, ketoprofen Oxaprozine, tiaprofen acid Naproxen ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C229/42C07C227/18A61K31/216A61P29/00
Inventor 王永生李桂英
Owner JILIN UNIV
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