反应详情

8-Methoxy-4-[[4-[[[1-(phenylmethyl)-4-piperidinyl]amino]carbonyl]phenyl]amino]-1-[[3-(trifluoromethyl)phenyl]methyl]-4-piperidinyl]-3-quinolinecarboxamide was prepared as a hygroscopic solid (0.46 hydrate) by coupling 8-methoxy-4-[[4-[[[1-(phenylmethyl)-4-piperidinyl]amino]carbonyl]phenyl]amino]-3-quinolinecarboxylic acid and 1-[[3-(trifluoromethyl)phenyl]methyl]-4-piperidinamine as described for Example 17, Step 5. 1-[[3-(trifluoromethyl)phenyl]methyl]-4-piperidinamine can be prepared from 3-(triflouromethyl)benzyl chloride and 1,4-dioxa-8-azaspiro[4.5]-decane as described in U.S. Pat. Nos. 3,875,165 and 4,816,464: mp 132°-138° C.; 1H NMR (Me2SO-d6, 400 MHz) δ 9.48 (s, 1 H), 8.76 (s, 1 H), 8.39 (d, J=7.6 Hz, 1 H), 7.97 (d, J=7.8 Hz, 1 H), 7.68 (d, J=8.7 Hz, 2 H), 7.10-7.65 (m, 12 H), 6.87 (d, J=8.7 Hz, 2 H), 3.94 (s, 3 H), 3.62-3.80 (m, 1 H), 3.35-3.60 (m, 5 H), 2.6-2.9 (m, 4 H), 1.95 (m, 4 H), 1.3-1.8 (m, 8 H); Karl Fischer, 0.46 moles of H2O.