反应详情

10-Bromo-2-carbamoyl-9-fluoro-5,6-dihydroimidazo[1,2-d][1,4]benzoxazepine-3-carboxylic acid (55 mg) was reacted with oxetan-3-ylmethanamine similar to as described in Example 2 to produce crude 10-bromo-9-fluoro-N3-(oxetan-3-ylmethyl)-5,6-dihydroimidazo[1,2-d][1,4]benzoxazepine-2,3-dicarboxamide which was then reacted with 2-Methyl-3-butyne-ol similar to as described in Procedure E to afford 13 mg of 9-fluoro-10-(3-hydroxy-3-methyl-but-1-ynyl)-N3-(oxetan-3-ylmethyl)-5,6-dihydroimidazo[1,2-d][1,4]benzoxazepine-2,3-dicarboxamide following reverse phase hplc purification. MS (Q1) 443 (M)+. 1H NMR (400 MHz, DMSO) δ 11.37 (t, 1H), 8.61 (d, J=8.4 Hz, 1H), 8.39 (s, 1H), 7.89 (s, 1H), 7.01 (d, J=10.5 Hz, 1H), 5.48 (s, 1H), 5.05-4.93 (m, 2H), 4.68-4.61 (m, 2H), 4.58-4.50 (m, 2H), 4.35 (t, J=6.0 Hz, 2H), 3.56 (t, J=6.1 Hz, 2H), 3.21-3.13 (m, 1H), 1.49 (s, 6H).