反应详情

温度

110 °C

A mixture of ethyl 1-cyclopropyl-6-fluoro-7-[4-(1,2,3-triazol-1-yl)piperidin-1-yl]-1,4-dihydro-4-oxo-1,8-naphthyridine-3-carboxylate (135 mg, 0.32 mmol) and 6N-HCl (6 ml) was heated at 110° C. for 18 hrs. The reaction mixture was concentrated and the residue was diluted with water. The pH of the suspension was adjusted to 7 by addition of NH4OH and this separated solid was filtered, washed with water, CH3CN and dried to give 60 mg of title product. m.p. 246°-248° C.; 1H NMR (TFA) δ: 9.25 (s, 1H), 8.65 (s, 1H), 8.52 (s, 1H), 8.25 (d, 1H), 5.35 (m, 3H), 4.12 (m, 1H), 3.75 (m, 2H), 2.40-2.85 (m, 4H), 1.25-1.70 (m, 4H).

1. concentrationThe reaction mixture was concentrated
2. additionthe residue was diluted with water
3. additionThe pH of the suspension was adjusted to 7 by addition of NH4OH
4. filtrationthis separated solid was filtered
5. washwashed with water, CH3CN
6. customdried