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Method for preparing etocoxib

A technology of etoricoxib and compounds, applied in the field of preparation of 5-chloro-3-phenyl-2-pyridine, which can solve the problems of toxic and harmful reagent use, waste generation, etc.

Inactive Publication Date: 2014-11-19
BEIJING VENTUREPHARM BIOTECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Patent EP0912518 synthesizes the target compound through palladium-catalyzed coupling of aryl / pyridyl halides with aryl / pyridyl boronic acid or stannane. This route involves such as Pd(PPH 3 ) 4 , OsO 4 The use of precious metal compounds, etc., will also have a large number of toxic and harmful reagents and waste generation

Method used

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Examples

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Embodiment

[0009] Step 1: Add 21.4 g of 4-methylsulfonylphenylacetic acid and 110 mL of methylene chloride to a 250 mL three-necked flask, stir at room temperature, measure 29 mL of thionyl chloride (about 47.6 g) and slowly add it dropwise to the reaction system, After the dropwise addition was completed, the reaction was stirred for 1 h; the reaction solution was evaporated to dryness at 50 °C to obtain an off-white solid; 100 mL of absolute ethanol was added to the off-white solid, and the solid was completely dissolved after stirring for 0.5 h; Concentrate to dryness by rotary evaporation to obtain an off-white product, which is dried at 40 °C for 12 h to obtain 23.9 g of compound 2 as a white solid with a yield of 98.76%.

[0010] Step 2: Add 12.1 g of compound 2 and 60 mL of tetrahydrofuran into a 250 mL three-necked flask, heat and stir, and control the temperature at 50 °C. Slowly add 50 mL of 2N tert-butylmagnesium chloride solution in tetrahydrofuran to the system, and heat for ...

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PUM

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Abstract

The invention relates to reparation of 5-chloro-3-(4-methylsulfonyl) phenyl-2-(2-methyl-5-pyridyl) pyridine which is a high-selectivity cycloxygenase-2(COX-2) inhibitor, has the functions of preventing inflammation, clearing heat, relieving pain and the like, has a very good curative effect on signs and symptoms of osteoarthritis in the acute stage and the chronic stage and on the acute gouty arthritis, and is an important non-steride anti-inflammatory medicine. According to the method, the medicine is prepped by virtue of three steps as shown in the specification by taking 4-methylsulfonyl phenylacetic acid as a raw material.

Description

Technical field [0001] The present invention is a pharmaceutical chemistry field, involving 5-chlorine-3- (4-sulfonic) benzene-2- (2-methyl-5-pyridin) pyridin preparation method.The purpose is to provide a simple, green, and high -end method to prepare for the past. Background technique [0002] Relying on Coscan is a high-selective epoxyase-2 (COX-2) inhibitor, which has the functions of anti-inflammatory, heating and analgesic.Flame medicine.Relying on Coscan, it was developed and developed by McFloros, Canada. It was first listed in Mexico in 2002. It has been listed in more than 70 countries such as the European Union other than the United States. [0003] At present, there is a relatively stable synthetic process relying on Coscan.Patent EP0912518 The target compounds are synthetic through the catalytic ster / pyridine halide and sterit / pyridine boric acid or izhanne. This route involves PD 3 Cure 4 , OSO 4 For the use of valuable metal compounds, there will also be a large n...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D213/61
Inventor 粟勇闫起强马苏峰
Owner BEIJING VENTUREPHARM BIOTECH
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