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Method for preparing felbinac

A technology of felbinac and biphenyl is applied in the field of preparation of non-steroidal anti-inflammatory drug felbinac, can solve problems such as being unsuitable for enterprise production, and achieve the effects of easy acquisition, simple operation and little environmental pollution

Inactive Publication Date: 2010-05-19
WUHAN INSTITUTE OF TECHNOLOGY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0015] To sum up, none of the above process routes is suitable for enterprise production

Method used

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  • Method for preparing felbinac

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] (1) Preparation of biphenyl chloride

[0036] On the 250ml three-necked flask, a thermometer, a mechanical stirrer, an air guide tube, and a reflux condenser were installed through a connecting pipe, and 15.4g (0.1mol) of biphenyl, 8.3g (0.1mol) of formaldehyde, 34.5g (0.3mol) of phosphoric acid, and Acetic acid 18.75g (0.3mol), concentrated hydrochloric acid 25ml. Heat to 80-90°C on an electronic thermostat heating mantle, stir vigorously for 18-24 hours, feed HCl gas into the reaction solution every 30 minutes, and the flow rate of hydrogen chloride gas is 45L / h. The reaction was stopped, cooled to below 15°C, and solids were precipitated. Filter under reduced pressure, wash the filter cake twice, each time about 40ml of water, and then use 20ml of 5% K 2 CO 3 The solution was washed once. Drain the filter cake, transfer it to a 250ml separatory funnel, add 40ml ether and 10ml 5% K 2 CO 3 The solution was shaken and left to stand, and the lye layer was separated...

Embodiment 2

[0042] (1) Preparation of diphenylchloromethane is the same as in Example 1.

[0043] (2) In a 250ml three-neck flask equipped with a condenser (with a calcium chloride drying tube attached to the top), a thermometer and an atmospheric dropping funnel, add 2.4g (0.1mol) of magnesium chips and 0.2g (0.002mol) of iodine crystals. . Measure 90ml of tetrahydrofuran, pour an appropriate amount of tetrahydrofuran just to cover the magnesium chips, and dissolve the remaining tetrahydrofuran with the biphenyl chloride methane obtained in the previous step, and put it in the normal pressure dropping funnel for use. Others are the same as above. 9.7 grams of felbinac crude product were obtained, and the total yield of the crude product was 45.6%.

[0044] (3) The refinement of felbinac was the same as that in Example 1. Recrystallization was carried out with 70% acetic acid to obtain 5.78 g of pure felbinac with a content of 99.79% and a melting point of 163-165° C. The yield of this ...

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Abstract

The invention relates to a preparation method of the biphenylacetic aicd of a non-steroidal anti-inflammatory drug, which includes two steps. The first step is to synthesize the biphenylacetic aicd, biphenyl is used as material, and a crude biphenylacetic aicd product is synthesized by chloromethylation, grignard reaction and hydrolysis, wherein, the molar ratio of the biphenyl, formaldehyde, phosphoric acid and acetic acid is 1:1:3:3, concentrated hydrochloric acid is overdosed, while the chloromethylation reacts, chlorine hydride gas is infused into reaction solution, and the flow of the chlorine hydride gas is 1 to 50l / h; the second step is refinement, the crude biphenylacetic aicd product produced in the first step is recrystallized by utilizing thirty to seventy percent (weight) of acetic acid solution, so that a pure biphenylacetic aicd product is produced. In the reaction process, the invention does not use and generate compounds with high toxicity and has little environmental pollution; materials can be easily got, and prices are low; all the used devices are conventional mechanical devices, operation is simple, and the total yield of crude products is thirty eight to fortysix persent.

Description

technical field [0001] The invention relates to the field of chemical synthesis medicine, in particular to a preparation method of felbinac, a non-steroidal anti-inflammatory drug. Background technique [0002] Felbinac is a non-steroidal anti-inflammatory drug. Its anti-inflammatory activity is similar to fenbufen. It has anti-inflammatory, analgesic and good transdermal properties. Its 3% gel ointment is widely used in osteoarthritis, frozen shoulder, Tenosynovitis, muscle pain, soft tissue injury, etc., have high effectiveness and safety. In September 1986, the Japanese Lederle Company's ointment under the trade name "Napageln" was launched in Japan for the first time. Later, the drug was launched in the UK under the trade name "Traxamgel". Currently, the drug has been listed in more than a dozen countries. According to domestic and foreign literature reports, there are more than ten synthetic routes of felbinac, including seven starting materials. For example: [0003...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07C57/38C07C51/15
Inventor 祝宏刘永琼潘盛钢高霞李胜松邹莹
Owner WUHAN INSTITUTE OF TECHNOLOGY
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