Process for production of 2-[4-(cyclopropanecarbonyl)phenyl]-2-methyl-propanenitrile

A technology of alkyl and phenyl, applied in the field of preparing 2-[4-(cyclopropanecarbonyl)phenyl]-2-methyl-propionitrile
CN107428678AActive Publication Date: 2017-12-01SANOFI AVENTIS DEUTSCHLAND GMBH
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Patent Information

Authority / Receiving Office
CN · China
Current Assignee / Owner
SANOFI AVENTIS DEUTSCHLAND GMBH
Publication Date
2017-12-01

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Abstract

A new process for the production of 2-[4-(cyclopropanecarbonyl)phenyl]-2-methyl- propanenitrile is described. This compound can be used for the production of drugs, such as Fexofenadine.
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Description

Background of the invention

[0001] The present invention relates to a chemical process for the preparation of 2-[4-(cyclopropanecarbonyl)phenyl]-2-methyl-propionitrile (compound of formula I) and its use as an intermediate for the preparation of medicines. For example, 2-[4-(cyclopropanecarbonyl)phenyl]-2-methyl-propionitrile is a key intermediate for the preparation of fexofenadine (compound of formula II).

[0002]

[0003] Fexofenadine II is an antihistamine drug used to treat allergic symptoms, and it is a bronchodilator (USP 4,254,129, Richardson-Merrell Inc.).

[0004] 2-[4-(Cyclopropanecarbonyl)phenyl]-2-methyl-propionitrile of formula I is an intermediate in the synthesis of fexofenadine and several prior art methods describe its preparation. These methods involve procedures using a large number of intermediates, as shown in Scheme 1 below, which summarizes this strategy. In USP 6,340,761 (Merrell Pharm. Inc.), the corresponding intermediates were prepared in Exam...

Claims

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