反应详情

A mixture of 132 mg of 2-benzyl-5-chloro-3-iodo-6-[(3R,4R)-3-hydroxy-4-methoxypyrrolidine-1-yl]pyridine, 49.4 mg of (3R)-3-ethynyl-3-quinuclidinol, 17.2 mg of tetrakis(triphenylphosphine)palladium(0), 11.3 mg of cuprous iodide, 124 μl of triethylamine and 1.5 ml of methanol was heated under reflux for one hour in a nitrogen atmosphere. After cooling as it was, water and ethyl acetate were added to the reaction mixture. The organic phase was washed with water and brine, dried over anhydrous magnesium sulfate and the solvent was removed. The residue was subjected to NH-silica gel column chromatography using 3% methanol/ethyl acetate, to give 125 mg of the target compound.

1. temperaturewas heated
2. temperatureunder reflux for one hour in a nitrogen atmosphere
3. temperatureAfter cooling as it
4. washThe organic phase was washed with water and brine
5. dry with materialdried over anhydrous magnesium sulfate
6. customthe solvent was removed