反应详情

Following the procedure as described in Example 16, making variations as required to replace N-benzyl-2-(3-(2,2-dimethoxyethyl)-3-(4-fluorobenzyl)ureido)-4-methylthiazole-5-carboxamide with 2-(3-(2,2-dimethoxyethyl)-3-(4-fluorophenethyl)ureido)-4-methyl-N-(pyridin-3-ylmethyl)thiazole-5-carboxamide, the title compound was obtained as a colorless solid in 21% yield: mp 182-184° C. (ethyl acetate); 1H NMR (300 MHz, CDCl3) δ 8.61-8.48 (m, 2H), 7.67 (d, J=7.2 Hz, 1H), 7.28 (br s, 1H), 7.18-7.03 (m, 2H), 6.97 (d, J=8.6 Hz, 2H), 6.12-5.93 (m, 2H), 4.72 (br s, 1H), 4.57 (d, J=5.7 Hz, 2H) 3.65-3.45 (m, 3H), 3.34-3.29 (m, 1H), 2.85 (t, J=7.2 Hz, 2H), 2.57 (s, 3H); 13C NMR (75 MHz, CDCl3) δ 162.3, 160.1, 157.1, 153.4, 153.3, 149.2, 149.0, 135.6, 133.6, 130.1, 130.0, 117.2, 115.7, 115.4, 77.2, 50.2, 44.8, 41.4, 33.1, 17.2; MS (ES+) m/z 456.3 (M+1).