Synthetic method of 2-(7-methoxyl-1-naphthyl) ethylamine hydrochloride

A technology of ethylamine hydrochloride and methoxy group is applied in the field of synthesis of 2-(7-methoxy-1-naphthyl)ethylamine hydrochloride, which can solve problems such as being difficult to realize industrialized production, and achieve the steps of Concise, high reaction yield, beneficial to the effect of industrialization promotion
CN103113243AInactive Publication Date: 2013-05-22SHANDONG FANGMING PHARMACEUTICAL CO LTD
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
SHANDONG FANGMING PHARMACEUTICAL CO LTD
Publication Date
2013-05-22
Estimated Expiration
Not applicable · inactive patent

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Abstract

The invention relates to a synthetic method of 2-(7-methoxyl-1-naphthyl) ethylamine hydrochloride. The method comprises the following steps of: reacting 7-methoxyl-1-naphthyl (a compound IV) with cyanoacetic acid to prepare (7-methoxyl-3,4-dihydro-1-naphthyl) acetonitrile (a compound III); performing deep drawing quality (DDQ) dehydrogenation to prepare (7-methoxyl-1-naphthyl) acetonitrile; using sodium borohydride as a reducing agent and reacting sodium borohydride with calcium chloride in anhydrous tetrahydrofuran to react to obtain 2-(7-methoxyl-1-naphthyl) ethylamine; and satisfying with hydrochloric acid to obtain a compound I, wherein the compound is an important intermediate of synthetic agomelatine.
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Description

technical field

[0001] The invention relates to a synthesis method of 2-(7-methoxy-1-naphthyl)ethylamine hydrochloride, belonging to the technical field of drug synthesis. Background technique

[0002] Depression (DEP) is a common mood disorder in psychiatry, with significant and persistent low mood as the main clinical feature, and the low mood is not commensurate with the situation. Clinically, it mainly includes: depression (severe depression), dysthymia, depression associated with brain or physical diseases, depression associated with mental disorders caused by psychoactive substances or non-addictive substances, and post-schizophrenia depression. Its clinical manifestations are depression, slow thinking, decreased speech and movement, and loss of interest in work. At least 10% of patients with depression may have manic episodes at different times in the future, and a diagnosis of bipolar disorder should be made at this time. Depression has become a major global mental...

Claims

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