アゴメラチン合成の新規な方法

Title:

アゴメラチン合成の新規な方法

Document Type and Number:

Japanese Patent JP5021004

Kind Code:

B2

Abstract:

Synthesis of agomelatine comprises reaction of 3-methoxyacenaphthoquinone (II) in the presence of strong base to obtain (7-methoxy-naphthalen-1-yl)-oxo-acetic acid (III); placing (III) under amination conditions to obtain 1-(7-methoxy-naphthalen-1-yl)-propane-1,2-dione (IV); reacting (IV) with a reducing system to obtain 2-(7-methoxy-naphthalen-1-yl)-ethylamine (V); and reacting (V) with sodium acetate and acetic anhydride to obtain agomelatine, which is isolated in the form of a solid. An independent claim is included for 1-(7-methoxy-naphthalen-1-yl)-propane-1,2-dione (IV) as intermediate for the synthesis of agomelatine. ACTIVITY : Antidepressant; Hypnotic; Cardiovascular-Gen.; Gastrointestinal-Gen.; CNS-Gen.; Eating-Disorders-Gen.; Anorectic; Muscular-Gen. MECHANISM OF ACTION : 5-Hydroxytryptamine 2C receptor antagonist.

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Inventors:

Christoph Arduin
Jean-Pierre Lukve

Application Number:

JP2009182087A

Publication Date:

September 05, 2012

Filing Date:

August 05, 2009

Export Citation:

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Assignee:

Réra Bora Toir Servier

International Classes:

C07C231/02; C07C209/68; C07C217/56; C07C233/22

Domestic Patent References:

JP2005247844A
JP9003016A
JP7048331A

Other References:

Tetrahedron Letters,1986年,Vol.27, No.32,pp 3775-3776

Attorney, Agent or Firm:

Hajime Tsukuni
Koshiro Tsukuda
Fusayuki Saito

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