New synthesizing process for modafinil

A technology of compound and reaction temperature, applied in the field of chemical synthesis of modafinil, namely 2-acetamide, can solve the problems of long reaction route, bad smell of diphenylmethane mercaptan, complicated operation and the like, and simplify the preparation and purification methods , Product yield and quality improvement, the effect of mild reaction conditions
CN1986527AInactive Publication Date: 2007-06-27浙江华纳药业有限公司
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Patent Information

Authority / Receiving Office
CN · China
Current Assignee / Owner
浙江华纳药业有限公司
Publication Date
2007-06-27
Estimated Expiration
Not applicable · inactive patent

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Abstract

The present invention discloses new process of synthesizing Modafinil, or 2-(diphenylmethyl sulfinyl) acetamide. The process includes the reaction of diphenyl methane as main material and bromine to obtain the intermediate diphenyl bromomethane, further condensation with mercapto acetic acid to obtain the intermediate diphenyl methylthio acetic acid, acyl chlorination to obtain the intermediate diphenyl methylthio acetyl chloride, amidation to obtain the intermediate diphenyl methylthio acetamide, and final sulfur-oxidation to obtain ultimate product Modafinil. The synthesis process of the present invention has facile material, mild reaction condition, relatively simple preparation and purification, and high product yield and quality, and is suitable for industrial production.
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Description

technical field

[0001] The invention relates to a new chemical synthesis method of modafinil (Modafinil, I), namely 2-(diphenylmethylsulfinyl)acetamide. Background technique

[0002] Modafinil (Modafinil, I) is the common name of 2-(diphenylmethylsulfinyl) acetamide, and its structural formula is as follows:

[0003]

[0004] Modafinil is a new type of refreshing drug that acts on the central nervous system developed by the French company Lafon. It was first launched in France in 1994. It is mainly used clinically for the treatment of narcolepsy and spontaneous hypersomnia.

[0005] Existing methods for the synthesis of modafinil have the following:

[0006] (1) The preparation methods disclosed in the patent Nos. DE 2809625, US 4177290A1 and US2002 / 0045629A1 use diphenylmethanol as a raw material to synthesize modafinil according to the following synthetic route (route 1).

[0007]

[0008] (2) The preparation method disclosed in the patent No. US 2004 / 002547A1 is c...

Claims

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