反应详情

Following the procedure as describe in preparation of Example 5, making variations as required to replace benzoyl chloride with 4-(trifluoromethoxy)benzoyl chloride to react with 2-amino-N-benzylisonicotinamide, N-benzyl-2-(4-trifluoromethoxybenzoylamino)isonicotinamide was obtained in 6% yield: mp 151-153° C.; 1H NMR (300 MHz, CDCl3) δ 8.83 (br s, 1H), 8.68 (s, 1H), 8.35 (d, J=5.0 Hz, 1H), 7.93 (d, J=9.0 Hz, 2H), 7.58-7.54 (m, 1H), 7.38-7.28 (m, 7H), 6.75 (br s, 1H), 4.64 (d, J=5.7 Hz, 1H); 13C NMR (75 MHz, CDCl3) δ 165.1, 164.5, 152.2, 151.8, 148.9, 144.2, 137.4, 132.0, 129.1, 128.8, 128.0, 127.8, 121.9, 120.8, 118.7, 118.5, 115.1, 110.5, 44.2; MS (ES+) m/z 416.4 (M+1).

1. customas describe in preparation of Example 5