Adamantane-1-carboxylic acid chloride (freshly prepared from the reaction of thionyl chloride (I) with the adamantane-1-carboxylic acid) was reacted with 1-(2-aminoethyl)-4-(2-pyrimidinyl)piperazine (II) in CH2Cl2 in the presence of triethylamine (TEA) to afford Wy-50,324 free base in 70% (III) yield which was converted to the hydrochloride salt using ethanolic HCl solution.