反应详情

A mixture of ethyl 1-cyclopropyl-6-fluoro-7-[3-(1,2,3-triazol-1-yl)piperidin-1-yl]-1,4-dihydro-4-oxo-1,8-naphthyridine-3-carboxylate (90 mg, 0.21 mmol) and 6N-HCl (5 ml) was heated to 100°-110° C. for 6 hrs. The mixture was concentrated and the residue was diluted with water. The pH of aqueous solution was adjusted to 7 by the addition of NH4OH and thus separated solid was filtered, washed with water, acetonitrile and dried to give 30 mg of desired product. m.p. 251°-254° C.; 1H NMR (TFA) δ: 9.25 (s, 1H), 8.65 (s, 1H), 8.55 (s, 1H), 8.22 (d, 1H), 5.37 (m, 1H), 5.15 (m, 1H), 4.38-4.75 (m, 2H), 4.10 (m, 2H), 2.45-2.85 (m, 2H), 2.00-2.40 (m, 2H), 1.22-1.65 (m, 4H).

1. temperaturewas heated to 100°-110° C. for 6 hrs
2. concentrationThe mixture was concentrated
3. additionthe residue was diluted with water
4. additionThe pH of aqueous solution was adjusted to 7 by the addition of NH4OH and thus separated solid
5. filtrationwas filtered
6. washwashed with water, acetonitrile
7. customdried