反应详情

A solution of ethyl 3-{[3-(ethyloxy)-3-oxopropanoyl][2-(2-oxo-1-pyrrolidinyl)ethyl]amino}-5-[(4-fluorophenyl)methyl]-2-pyridinecarboxylate (1.80 g, 3.98 mmol) in ethanol (20 mL) was treated with DBU (1.53 mL, 10.3 mmol). After stirring under nitrogen for 20 min., the reaction was quenched with 1N HCl (7.8 mL) and evaporated in vacuo. Trituration with water and filtration provided the product as a white solid: 1H NMR (CDCl3) δ 8.50 (1H, d, J=1.4 Hz), 8.11 (1H, s), 7.26 (2H, m), 7.00 (2H, ddd, J˜9, 9, 2 Hz), 4.52 (2H, q, J=7 Hz), 4.33 (2H, br t, J˜7 Hz), 4.14 (2H, s), 3.52-3.44 (4H, m), 2.35 (2H, t, J=8 Hz), 2.00 (2H, m), 1.48 (3H, t, J=7 Hz); ES+ MS: 476 (M+Na+).

1. customthe reaction was quenched with 1N HCl (7.8 mL)
2. customevaporated in vacuo
3. filtrationTrituration with water and filtration