反应详情

Following the procedure as described in Example 9, making variations only as required to use 1-(bromomethyl)-4-(difluoromethoxy)benzene in place of 2-cyclopropylethyl 4-methylbenzenesulfonate to react with N-benzyl-5-(4-hydroxy-2-oxopyridin-1(2H)-yl)-3-methylthiophene-2-carboxamide, the title compound was obtained as a pinkish solid in 35% yield: mp 178-180° C.; 1H NMR (300 MHz, DMSO-d6) δ 8.55 (t, J=6.0 Hz, 1H), 8.16 (d, J=8.0 Hz, 1H), 7.53 (d, J=8.5 Hz, 2H) 7.38-7.20 (m, 9H), 6.28 (dd, J=7.9, 2.7 Hz, 1H), 6.14 (d, J=2.7 Hz, 1H), 5.16 (s, 2H), 4.41 (d, J=6.0 Hz, 2H), 2.42 (s, 3H); 13C NMR (75 MHz, DMSO-d6) δ 166.1, 162.4, 160.9, 150.8, 139.6, 138.8, 137.2, 135.1, 132.4, 129.9, 128.2, 127.3, 127.4, 127.1, 126.6, 120.6, 118.7, 116.2, 102.5, 97.3, 69.2, 42.5, 15.5; MS (ES+) m/z 497.3 (M+1).