Serotonergic agents with long-acting in vivo effects
a serotonergic agent and in vivo technology, applied in the field of serotonergic agents with long-acting in vivo effects, can solve problems such as schizophrenia and alzheimer's disease treatmen
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example 1
1-Methyl-cyclohexanecarboxylic acid {(1R)-1-cyclohexylmethyl-2-[4-(2-methoxy-phenyl)-piperazin-1-yl]-ethyl}-amide hydrochloride hydrate
[0033] To a solution of 0.30 g (0.91 mmol) of {(1R)-1-cyclohexylmethyl-2-[4-(2-methoxyphenyl)-piperazin-1-yl]-ethyl}-amine and 0.25 mL (1.74 mmol) of triethyl-amine in 10 mL of dichloromethane at 0° C. was added dropwise 0.16 g (1.00 mmol) of 1-methylcyclohexane-carboxylic acid chloride in 4 mL of dichloromethane. The reaction mixture was allowed to stir under nitrogen at 0° C. for one hour, and was then concentrated on a rotary evaporator, diluted with ethyl acetate and washed with saturated aqueous NaHCO3 and brine. The organic phase was dried over anhydrous sodium sulfate, filtered and concentrated on a rotary evaporator to yield the crude product, which was purified by flash chromatography on silica gel (dichloro-methane / methanol) and then converted to the hydrochloride.hydrate salt of the title compound with ethanolic HCl to yield 0.30 g (63%) ...
example 2
[Methoxy-3H]-1-Methyl-cyclohexanecarboxylic acid {(1R)-1-cyclohexylmethyl-2-[4-(2-methoxy-phenyl)-piperazin-1-yl]-ethyl}-amide hydrochloride hydrate
[0035] Sodium hydride is added to a solution of 1-Methyl-cyclohexanecarboxylic acid {(1R)-1-cyclohexylmethyl-2-[4-(2-hydroxyphenyl)-piperazin-1-yl]-ethyl}-amide in DMF and the solution is stirred at room temperature under nitrogen for 2 hours. [3H] methyl iodide is added to the reaction mixture which is stirred at room temperature for 1.5 hours. The reaction mixture is pumped to dryness on the manifold and taken to dryness several times with ethanol.
example 3
[Methoxy-11C]1-Methyl-cyclohexanecarboxylic acid {(1R)-1-cyclohexylmethyl-2-[4-(2-methoxy-phenyl)-piperazin-1-yl]-ethyl}-amide hydrochloride hydrate
[0036] In a suitable manifold, sodium hydride is added to a solution of 1-Methyl-cyclohexanecarboxylic acid {(1R)-1-cyclohexylmethyl-2-[4-(2-hydroxy-phenyl)-piperazin-1-yl]-ethyl}-amide in dimethylformamide under nitrogen. [11C]-methyl iodide is distilled into the reaction mixture and the reaction is heated to 80° C. for 5 minutes. After purification by HPLC the material is formulated for i.v. injection by dissolution in normal saline and sterile millipore filtration.
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