反应详情

2-[1-Benzoyl-3-(3,4-dichloro-phenyl)-pyrrolidin-3-yl]ethyl methanesulfonate (191 mg, 0.43 mmol) was treated with the 4-phenyl-piperidine-4-carboxylic acid amide hydrochloride (144 mg, 0.599 mmol) and NaHCO3 (90 mg, 1.07 mmol, 2.5 eq.) in THF/H20 (5 mL/1 mL) at reflux for 21 hours. The solution was concentrated in vacuo and the aqueous phase was extracted with dichloromethane. The organic phase was dried over magnesium sulfate, filtered, and concentrated in vacuo. The residue was chromatographed on silica gel (30 g) with 6% methanol in dichloromethane to give 146 mg (44%).

1. temperatureat reflux for 21 hours
2. concentrationThe solution was concentrated in vacuo
3. extractionthe aqueous phase was extracted with dichloromethane
4. dry with materialThe organic phase was dried over magnesium sulfate
5. filtrationfiltered
6. concentrationconcentrated in vacuo
7. customThe residue was chromatographed on silica gel (30 g) with 6% methanol in dichloromethane
8. customto give 146 mg (44%)