反应详情

To a solution of the product from the Example 28A (0.182 g, 0.6 mmol) in N,N-dimethylformamide (5 mL) was added 1-(2-bromoethyl)-3,3-diphenylpyrrolidin-2-one (Example 64B, 0.2 g, 0.6 mmol), potassium carbonate (0.25 g, 1.8 mmol), and a catalytic amount of potassium iodide. The reaction mixture was stirred at room temperature overnight. The reaction mixture was concentrated in vacuo, and partitioned in H2O/dichloromethane. The organic layer was separated, dried over MgSO4, and concentrated. The obtained residue was chromatographed eluting with 5% methanol/dichloromethane to yield the title compound. 1H NMR (300 MHz, CDCl3) δ ppm 7.31 (m, 10H), 7.20 (m, 11H), 3.50 (t, J=6.10 Hz, 2H), 3.38 (t, J=6.44 Hz, 2H), 3.33 (m, 2H), 3.00 (m, 2H), 2.71 (m, 4H), 2.58 (t, J=6.27 Hz, 2H), MS (ESI+) m/z 530 (M+H)+.

1. concentrationThe reaction mixture was concentrated in vacuo
2. custompartitioned in H2O/dichloromethane
3. customThe organic layer was separated
4. dry with materialdried over MgSO4
5. concentrationconcentrated
6. customThe obtained residue was chromatographed
7. washeluting with 5% methanol/dichloromethane