3,4-Difluorobenzylamine → N-(3,4-Difluorobenzyl)-2-(4-hydroxy-2-oxopyridin-1(2H)-yl)-4-methylthiazole-5-carboxamide

Beteiligte Stoffe

Reaktionsschritte

Following the procedure as described in Example 1, making variations only as required to use 2-(4-hydroxy-2-oxopyridin-1(2H)-yl)-4-methylthiazole-5-carboxylic acid in place of 4-methyl-2-(2-oxo-4-phenylpyridin-1(2H)-yl)thiazole-5-carboxylic acid to react with (3,4-difluorophenyl)methanamine, the title compound was obtained as a colorless solid in 88% yield: mp 294-296° C. (ethyl acetate/hexanes); 1H NMR (300 MHz, DMSO-d6) δ 11.50 (br s, 1H), 8.77 (t, J=5.8 Hz, 1H), 8.59 (d, J=8.0 Hz, 1H), 7.40-7.28 (m, 2H), 7.15-7.10 (m, 1H), 6.26 (dd, J=8.0, 2.6 Hz, 1H), 5.82 (d, J=2.6 Hz, 1H), 4.35 (d, J=5.8 Hz, 2H), 2.53 (s, 3H); 13C NMR (75 MHz, DMSO-d6) δ 167.9, 162.1, 161.6, 154.2, 150.5, 137.7, 132.6, 124.5, 123.3, 117.8, 117.6, 116.8, 116.6, 104.4, 98.0, 42.2, 17.5; MS (ES+) m/z 378.2 (M+1).

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