Adatanserin hydrochloride

Originator

WY-50324 ,Centre de Recherche Pierre Fabre

Manufacturing Process

To a stirred solution of [4-(2-pyrimidinyl)piperazino]ethylamine (2.0 g, 0.01 mol) in 50 ml of methylene chloride, adamantane-1-carboxylic acid chloride (3.6 g, 0.018 mol) and triethylamine (2.9 g, 0.015 mol) were added. Stirring was continued at room temperature overnight. The methylene chloride solution was washed with water, dried over anhydrous sodium sulfate and evaporated under reduced pressure. The remaining residue was subjected to preparative HPLC. The residue was dissolved in ethyl acetate (10 ml) and subjected to flash chromatography using a 9 inch column of silica gel and ethyl acetate as the eluent. The N-[2-[4-(2-pyrimidinyl)-1- piperazinyl]ethyl]tricyclo[3.3.1.1(3,7)] decane-1-carboxamide was separated.
In practice it is usually used as hydrochloride.

Therapeutic Function

Anxiolyticá Antidepressant

Raw materials

Preparation Products