Method for preparing modafinil

A diphenylmethyl, thio-based technology, applied in the field of preparing high-purity modafinil, can solve problems such as tediousness, unsatisfactory yield and the like

Inactive Publication Date: 2013-08-14
重庆凯林制药有限公司 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

This method can be said to be effective, but it is a bit cumbersome, and the yield is not ideal, up to 85%

Method used

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  • Method for preparing modafinil
  • Method for preparing modafinil
  • Method for preparing modafinil

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Embodiment Construction

[0029] According to the method of the present invention, the peroxidation reaction in the preparation process of the crude modafinil must be avoided in order to prepare modafinil meeting the requirements of medicinal purity, because the product sulfone of the peroxidation reaction is difficult to remove from the finished product. Based on this consideration, the present invention attempts to reduce the concentration of oxidant hydrogen peroxide to avoid the generation of peroxidation reaction. After a large number of experiments, it was found that the reaction of hydrogen peroxide in a mixed system composed of water and glacial acetic acid can well avoid peroxidation. The following table briefly illustrates the influence of different proportions of water and glacial acetic acid on the purity of the finished product and the oxidation yield:

[0030]

[0031] Wherein lot number 20070101 is the result of repeating Example 1 of the '290 patent.

[0032] Finally, the following ...

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Abstract

A method for producing armodafinil is provided. The method comprises the following steps: firstly, hydrogen peroxide is used to oxidize Bis-[(diphenyl methyl) thio]acetamide to form a crude product of armodafinil and, secondly the armodafinil produced in step 1 is re-crystallized with absolute ethanol to form an armodafinil meeting the requirement on the purity. The method has the advantages thatthe substitution of a mixture system of water and acetic acid glacial for the pure acetic acid glacial in the embodiment of invention 290 avoids satisfactorily the peroxidation in the process of oxidation, and that the yield of the oxidation is improved dramatically. The method can produce the armodafinil meeting the requirement on purity with the produced crude product of armodafinil through thesimple re-crystallization.

Description

technical field [0001] The invention belongs to the field of pharmacy and relates to a method for preparing high-purity modafinil. It specifically relates to the oxidation of 2-[(diphenylmethyl)thio]acetamide with hydrogen peroxide in a system composed of glacial acetic acid and water to obtain the crude modafinil, which is obtained by recrystallization of the crude modafinil by an appropriate method. Method for modafinil meeting pharmaceutical purity requirements. Background technique [0002] Modafinil (Formula 1), chemical name (±) 2-[(diphenylmethyl)sulfinyl]acetamide, has the effect of promoting insomnia on humans and animals. [0003] [0004] The psychotropic activity of modafinil was demonstrated in animal tests and clinical experiments on human patients as described in US Patent No. 4,177,290 (the "'290 patent"). FDA approves modafinil racemate for the treatment of narcolepsy. [0005] The '290 patent describes the preparation of modafinil. In Example 1 of...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07C317/44C07C315/02
Inventor 龙道兵左小勇姚全兴杨洋曹晓红游伟杨毅
Owner 重庆凯林制药有限公司
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