2-(1-(4-fluorobenzyl)-5-oxo-1H-1,2,4-triazol-4(5H)-yl)-4-methylthiazole-5-carboxylic acid → N-((1H-pyrazol-3-yl)methyl)-2-(1-(4-fluorobenzyl)-5-oxo-1H-1,2,4-triazol-4(5H)-yl)-4-methylthiazole-5-carboxamide

Participants

Reaction Steps

Following the procedure as described in Example 21, making variations as required to replace 4-methyl-2-(5-oxo-1-(4-(trifluoromethyl)benzyl)-1H-1,2,4-triazol-4(5H)-yl)thiazole-5-carboxylic acid with 2-(1-(4-fluorobenzyl)-5-oxo-1H-1,2,4-triazol-4(5H)-yl)-4-methylthiazole-5-carboxylic acid to react with (1H-pyrazol-3-yl)methanamine, the title compound was obtained as a white solid in 49% yield: mp 178-179° C. (ethyl acetate/hexane); 1H NMR (300 MHz, CDCl3) δ 8.23 (s, 1H), 7.59 (br s, 1H), 7.39-7.30 (m, 2H), 7.06-6.96 (m, 2H), 6.88 (t, J=4.7 Hz, 1H), 6.33 (br s, 1H), 6.05 (br s, 1H), 4.95 (s, 2H), 4.64 (d, J=4.7 Hz, 2H), 2.63 (s, 3H); MS (ES+) m/z 414.2 (M+1).

Provenance & Evidence