N-Methylbenzylamine → HCID 86751299, compound

Participants

Reaction Steps

To a stirred mixture of (2R)-1-[3,5-bis(trifluoromethyl)benzoyl]-2-(3,4-dimethylbenzyl)-4-(carboxymethyl)piperazine hydrochloride (210 mg), N-methylbenzylamine (52 mg) and triethylamine (0.19 ml) in dichloromethane (5 ml) was added 2-chloro-1-methylpyridinium iodide (110 mg) under nitrogen atmosphere at room temperature. The mixture was stirred at the same temperature for 1 hour. After removal of the solvent, the residue was purified by column chromatography on a silica gel eluting with a mixture of dichloromethane and methanol (10:1). The eluate was concentrated and treated with 4N hydrogen chloride in ethyl acetate solution to give (2R)-1-[3,5-bis(trifluoromethyl)benzoyl]-2-(3,4-dimethylbenzyl)-4-[(N-methyl-N-benzylcarbamoyl)methyl]piperazine hydrochloride (190 mg) as a powder.

Provenance & Evidence