It is an antidepressants, NEUROLOGIC DRUGS,PSYCHOPHARMACOLOGIC DRUGS,MAO-A Inhibitors.
is used for the treatment of Cognition Disorders, and Mood Disorders.
Bromination of 2-hydroxy-5-methoxybenzaldehyde (I) in acetic acid / sodium acetate mixture gives bromoaldehyde (II). Condensation to the benzofuranylpyridine (IV) is achieved by heating a solution of (II) and 4-(chloromethyl)pyridine hydrochloride (III) in polyethylene glycol-400 in the presence of potassium carbonate. Quaternization of (IV) with dimethylsulfate in dichloromethane affords (V), which upon reduction with sodium borohydride gives intermediate (VI). Reduction of (VI) with platinum on charcoal in methanol/HBr solution yields the N-methylpiperidine (VII). Degradation of the N-methyl group with ethylchloroformate in toluene affords the carbamate (VIII). Final treatment of (VIII) with potassium hydroxide in n-butanol yields the free base of brofaremine, which is converted to its hydrochloride salt by treatment with hydrochloric acid in methanol.
1. | orl-rat LD50:310 mg/kg | DRFUD4 Drugs of the Future. 10 (1985),371. | ||
2. | orl-mus LD50:190 mg/kg | DRFUD4 Drugs of the Future. 10 (1985),371. | ||
3. | orl-dog LD50:100 mg/kg | DRFUD4 Drugs of the Future. 10 (1985),371. |
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