反应详情

To the solution of tert-butyl 4-{[5-(2-chlorophenyl)-1-(2,6-dichlorophenyl)-2-oxo-1,2,3,4-tetrahydroquinazolin-7-yl]methyl}-1-isopropylpiperazine-2-carboxylate (EXAMPLE AAA11, 30 mg, 0.047 mmol) in trifluoroacetic acid (0.6 mL) was added water (0.03 mL). The reaction was stirred at rt for 20 h. Removal of the solvent and subsequent addition of ether resulted in a white precipitate. Filtration of the precipitate followed by washing with ether provided the title compound. 1H NMR (CDCl3, 500 MHz): δ 1.22 (d, 3H, J=7.0 Hz), 1.24 (d, 3H, J=6.9 Hz), 3.12(m, 2H), 3.30 (m, 1H), 3.44 (m, 1H), 3.50 (abq, 2H, J=7.1 Hz), 3.74 (m, 1H), 3.81 (m, 1H), 3.96 (m, 1H), 4.07 (m, 1H), 4.28 (dd, 1H, J1=14.6 Hz, J2=5.7 Hz), 4.42 (dd, 1H, J1=14.9 Hz, J2=10.1 Hz), 5.80 (brs, 1H), 6.13 (d, 1H, J=9.8 Hz), 6.95 (s, 1H), 7.32-7.58 (m, 7H). MS (API-ES+): 589 (M+H).

1. customRemoval of the solvent and subsequent addition of ether
2. customresulted in a white precipitate
3. filtrationFiltration of the precipitate
4. washby washing with ether