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A kind of preparation method and important intermediate of bromfenac sodium

A technology of bromfenac sodium and intermediates, which is applied in the field of drug synthesis, can solve the problems of affecting the therapeutic effect of products, less bromfenac sodium, and high toxicity, and achieve the effects of cheap and easy reagents, less environmental pollution, and easy purification

Active Publication Date: 2018-05-18
TIANJIN JINYAO GRP
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] In addition, there are few reports on the refining of bromfenac sodium at present, and the method reported in the literature is to use 1,2-dimethoxyethane as the refining solvent
1,2-Dimethoxyethane is a second-class solvent specified by ICH. It is highly toxic and is a restricted solvent. Its residue in the finished product of bromfenac sodium will cause harm to the human body, thus affecting the therapeutic effect of the product

Method used

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  • A kind of preparation method and important intermediate of bromfenac sodium
  • A kind of preparation method and important intermediate of bromfenac sodium
  • A kind of preparation method and important intermediate of bromfenac sodium

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028]

Embodiment 1-1

[0030] Under nitrogen protection, add 107g of acetaminobenzenesulfonic acid to a 1L reaction flask, add 537ml of dichloromethane to dissolve, add 41.5g of chloroacetonitrile, add 13.6g of zinc chloride in batches, heat to 40°C, reflux for 2 hours, and detect by TLC After the reaction is complete, cool to room temperature. Slowly add 3ml of water dropwise to the reaction solution, and control the temperature of the ice-salt bath to less than 20°C. The insoluble matter was removed by filtration, and the filtrate was washed with water until neutral, then concentrated to near dryness under reduced pressure. The obtained crude product was recrystallized from ethyl acetate to obtain 94 g of white solid, with a yield of 74%.

[0031] Examples 1-2 to 1-24 Refer to Example 1-1 for the amount of starting material and operation steps, and refer to the table below for other conditions. The experimental results are shown in the table below:

[0032]

[0033]

[0034] Compound II: m...

Embodiment 2

[0039]

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PUM

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Abstract

The invention provides a method for preparing and refining bromfenac sodium which is mild in reaction conditions, simple in operation, high in purity, high in yield, low in cost and easy for industrial production.

Description

technical field [0001] The invention belongs to the field of drug synthesis, and relates to a new method for preparing non-steroidal anti-inflammatory drug bromfenac sodium and an important intermediate thereof. Background technique [0002] Bromfenac sodium (Bromfenac sodium, chemical name: 2-amino-3-(4-bromobenzoyl) phenylacetate sodium), is a non-steroidal anti-inflammatory drug developed by Wyeth-Ayerst Company, which has a strong analgesic effect , launched in the United States in 1997, is used to treat sharp pain without addiction. Subsequently, it was developed and marketed as eye drops by Japan's Chishou Company for the symptomatic treatment of inflammatory diseases of the outer eye and anterior eye: blepharitis, conjunctivitis, dynastic inflammation (including superior dynastic inflammation), postoperative inflammation, etc. . The drug has an outstanding therapeutic effect on eye postoperative inflammation, is well tolerated, has no effect on intraocular pressure,...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07C229/42C07C227/00C07C309/61
Inventor 顾艳艳张杰
Owner TIANJIN JINYAO GRP
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