反应详情

To a solution of rac-6-chloro-3-(3-chloro-benzyl)-3-piperidin-3-yl-1,3-dihydro-indol-2-one (80 mg, 0.21 mmol) (from Example 25a supra) in dichloromethane (3 mL) was added triethylamine (74.3 ul, 0.53 mmol) (Aldrich), followed by the addition of solution of 4-isocyanato-pyridine (1.28 mL, 0.26 mmol) in toluene (from Example 58a supra). The mixture was stirred at room temperature for 30 minutes. The mixture was partitioned between dichlormethane and water. The aqueous layer was extracted with dichlormethane. The combined organic layer was washed with water, brine, dried over Na2SO4 and concentrated. The residue was purified by chromatography to give rac-3-[6-chloro-3-(3-chloro-benzyl)-2-oxo-2,3-dihydro-1H-indol-3-yl]-piperidine-1-carboxylic acid pyridine-4-ylamide as a white solid. (Yield 23 mg, 21.9%).

1. customThe mixture was partitioned between dichlormethane and water
2. extractionThe aqueous layer was extracted with dichlormethane
3. washThe combined organic layer was washed with water, brine
4. dry with materialdried over Na2SO4
5. concentrationconcentrated
6. customThe residue was purified by chromatography