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Process for synthesizing sertaconazole

A kind of technology of sertaconazole nitrate and synthetic method, applied in directions such as organic chemistry, can solve problems such as trivial reaction, high price, difficult conditions, etc., and achieve the effects of easy operation, low cost and stable yield

Inactive Publication Date: 2005-03-02
河北省药物研究所
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  • Abstract
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Problems solved by technology

[0007] 3. The used hexamethylphosphoric triamide is toxic and expensive;
[0008] 4. The reaction is cumbersome, the conditions are difficult to control, and the cost is high

Method used

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  • Process for synthesizing sertaconazole
  • Process for synthesizing sertaconazole

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Embodiment

[0018] 1), 0.2mol of 1-(2,4-dichlorobenzene)-2-(1-imidazole)ethanol, 0.2mol of 3-bromomethyl-7-chlorobenzo [b] thiophene, 12g of hydroxide Dissolve sodium and 16ml of 50% tetrabutylammonium chloride aqueous solution in 240ml of toluene and 80ml of water, heat up to 80°C, stir at constant temperature for 4 hours, and cool;

[0019] 2), add 80ml of water, then extract several times with 4L ether, combine the organic layers, dry with anhydrous sodium sulfate, and filter;

[0020] 3), add 12ml concentrated nitric acid under stirring at room temperature, precipitate solid, filter;

[0021] 4) Recrystallized with 95% ethanol and dried under reduced pressure to obtain 59 g of white solid sertaconazole nitrate, yield 59%, mp 157-158°C.

[0022] The reaction of the present invention is as follows:

[0023]

[0024] Compared with the synthetic method of the prior art, the present invention has the following advantages:

[0025] 1. The present invention utilizes phase transfer cata...

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Abstract

The present invention provides a phase transfer catalytic synthesis method of shetaconzole nitrate, said method includes: using 1-(2,4-dichlorophenyl)-2-(1-imidazole) ethyl alcohol and 3-bromomethyl-7-chlorobenzo [b] thiophene as raw material, using methylbenzene and water as solvent and using tetrabutyl ammonium chloride as catalyst, in the presence of sodium hydroxide making phase transfer catalytic reaction to prepare shetaconzole nitrate. Said ivnention is simple and convenient in operation, and utilizes element analysis, infrared spectrum, NMR hydrogen spectrum, NMR carbon spectrum and mass spectrum to confirm its chemical structure, its content is greater than 98.5%.

Description

technical field [0001] The invention relates to a synthesis method of sertaconazole nitrate, belongs to the technical field of organic synthesis, and is suitable for preparing pharmaceutical raw materials or intermediates. Background technique [0002] Topical antifungal drug Sertaconazole Nitrate (Sertaconazole Nitrate), molecular formula: C 20 h 15 Cl 3 N 2 OS·HNO 3 , developed by Spain, and applied for patents in many countries, such as ES8504779, EP151477, ES535656, JP60 / 181086, US5135943, etc., its synthetic route uses 1-(2,4-dichlorobenzene)-2-(1-imidazole) Ethanol and 3-bromomethyl-7-chlorobenzo[b]thiophene are used as raw materials, react with sodium hydride under the protection of inert gas to obtain sertaconazole, and then prepare nitrate. The reaction formula is as follows: [0003] [0004] The weak point of above-mentioned synthesis method is: [0005] 1. The reaction needs to be completed under the protection of inert gas; [0006] 2. The sodium hydr...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D409/12
Inventor 陈宝泉赵煜松马宁曾海霞
Owner 河北省药物研究所
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