反应详情

Following the procedure as described in Example 3, making variations only as required to use pyridin-2(1H)-one in place of 4-aminopyridin-2(1H)-one to react with 2-bromo-N-(4-fluorobenzyl)-4-methylthiazole-5-carboxamide in place of N-benzyl-2-bromo-4-methylthiazole-5-carboxamide, the title compound was obtained as a colorless solid in 45% yield: mp 170-172° C. (hexane/ethyl acetate); 1H NMR (300 MHz, CDCl3) δ 8.80-8.77 (m, 1H), 7.47-7.42 (m, 1H), 7.34-7.28 (m, 2H), 7.03 (t, J=8.6 Hz, 2H), 6.75 (d, J=9.4 Hz, 1H), 6.44 (d, J=6.9 Hz, 1H), 6.06 (t, J=5.6 Hz, 1H), 4.56 (d, J=5.6 Hz, 2H), 2.70 (s, 3H); 13C NMR (75 MHz, CDCl3) δ 163.9, 162.1, 160.6, 153.2, 152.5, 139.9, 133.5, 131.2, 129.6, 129.5, 122.9, 121.3, 115.8, 115.5, 107.8, 43.4, 17.3; (ES+) m/z 344.2 (M+1).