反应详情

To a solution of 5-butyl-1-(5-methyl-4-(thiazol-5-yl)pyrimidin-2-yl)-1H-pyrazole-4-carboxylic acid (72 mg, 0.21 mmol), 5,6,7,8-tetrahydro-[1,2,4]triazolo[4,3-a]pyrazine (50 mg, 0.23 mmol), HBTU (119 mg, 0.32 mmol) and 4 mL of DMF was added DIEA (54 μL, 0.73 mmol). The reaction was stirred at room temperature for 2 hours at which time the crude mixture was purified directly by reverse phase preparative HPLC to provide 3.0 mg of 30 as a white solid. 1H NMR (400 MHz, MeOD-d3) δ 0.78 (t, J=7.2 Hz, 3H), 1.35 (m, 2H), 1.61 (m, 2 H), 2.69 (s, 3H), 3.4 (t, J=7.7 Hz, 2H), 4.18 (t, J=5.1 Hz, 2H), 4.31 (t, J=5.5 Hz, 2H), 5.10 (s, 2H), 7.32 (t, J=4.5 Hz, 1H), 7.82 (d, J=5.1 Hz, 1H), 7.96 (s, 1H), 7.99 (d, J=2.7 Hz, 1H), 8.54 (s, 1H), 8.76 (s, 1H). LCMS (ES+) m/z 449 (M+1).

1. customwas purified directly by reverse phase preparative HPLC