反应详情

2-carbamoyl-9-fluoro-10-(3-hydroxy-3-methyl-but-1-ynyl)-5,6-dihydroimidazo[1,2-d][1,4]benzoxazepine-3-carboxylic acid (0.05 g) was reacted with 1-pyrrolidineethylamine similar to as described in Example 2 to afford 21.1 mg of 9-fluoro-10-(3-hydroxy-3-methyl-but-1-ynyl)-N3-(2-pyrrolidin-1-ylethyl)-5,6-dihydroimidazo[1,2-d][1,4]benzoxazepine-2,3-dicarboxamide following reverse phase hplc purification. MS (Q1) 470 (M)+. 1H NMR (400 MHz, DMSO) δ 11.20 (t, J=5.5 Hz, 1H), 8.61 (d, J=8.4 Hz, 1H), 8.42 (s, 1H), 7.90 (s, 1H), 7.03 (d, J=10.5 Hz, 1H), 5.47 (s, 1H), 5.02-4.84 (m, 2H), 4.64-4.43 (m, 2H), 3.65-3.49 (m, 2H), 3.16-2.81 (m, 6H), 1.95-1.79 (m, 4H), 1.49 (s, 6H).