Ethyl Acetate → (R)-1-[2-[3-(3,4-dichloro-phenyl)-1-(3,4,5-trimethoxy-benzoyl)-pyrrolidin-3-yl]-ethyl]-4-(pyridin-3-yl)-piperidine-4-carboxylic acid 4-methylpiperazine-amide

Participants

Reaction Steps

Prepare by the method of Example 88.6 using (S)-2-[1-(3,4,5-trimethoxy-benzoyl)-3-(3,4-dichloro-phenyl)-pyrrolidin-3-yl]-ethyl-methanesulfonate and 4-(pyridin-3-yl)-piperidine-4-carboxylic acid 4-methylpiperazine-amide to give, after chromatography on silica gel eluting sequentially with ethyl acetate, 1% methanol/dichloromethane, 3% methanol/dichloromethane, 5% methanol/dichloromethane, 7% methanol/dichloromethane, and then 9% methanol/dichloromethane, the title compound: Rf =0.29 (silica gel, methanol/dichloromethane/concentrated ammonia 10/90/0.5).

Provenance & Evidence