反应详情

To a solution of aripiprazole (1.5 g, 3.35 mmol) in dichloromethane (33 mL) was added triethylamine (0.56 mL, 4.01 mmol) and benzyl isocyanate (0.82 mL, 6.69 mmol). The reaction was stirred at room temperature for 48 hours. The reaction was quenched with water and extracted with dichloromethane (3×20 mL). The organics were combined, washed with brine (20 mL), dried over MgSO4 and concentrated. The residue was purified by column chromatography on silica eluting with 0-10% tetrahydrofuran in ethyl acetate. The product was triturated in heptane to remove aliphatic impurities and then filtered and dried to afford Compound-79 (0.575 g) as a colorless solid.

1. customThe reaction was quenched with water
2. extractionextracted with dichloromethane (3×20 mL)
3. washwashed with brine (20 mL)
4. dry with materialdried over MgSO4
5. concentrationconcentrated
6. customThe residue was purified by column chromatography on silica eluting with 0-10% tetrahydrofuran in ethyl acetate
7. customThe product was triturated in heptane
8. customto remove aliphatic impurities
9. filtrationfiltered
10. customdried
11. customto afford Compound-79 (0.575 g) as a colorless solid