| 摘要 |
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)-pr opane-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. |
