反应详情

To a solution of 5-[5-(4-methoxy-phenyl)-pyrimidin-2-ylamino]-pyridine-2-carboxylic acid 5 (0.05 mmol) in DMF (1 mL) is added HATU (0.06 mmol) and DIEA (0.14 mmol) at rt. The resulting mixture is stirred for 2 min and then piperazine-2-one (0.05 mmol) is added. The reaction mixture is stirred at it for 12 h and then directly purified by preparative LCMS to give 4-{5-[5-(4-methoxy-phenyl)-pyrimidin-2-ylamino]pyridine-2-carbonyl}-piperazin-2-one A2 as a white solid. 1H NMR (400 MHz, d4-CH3OH) δ 8.98 (d, J=4.0 Hz, 1H), 8.77 (s, 1H), 8.53-8.52 (m, 2H), 7.74-7.73 (m, 2H), 7.58-7.56 (m, 2H), 7.07-7.05 (m, 2H), 3.94 (bs, 2H), 3.81 (s, 3H), 3.46 (bs, 2H), 3.45 (bs, 2H). MS (m/z) (M+1)+: 405.2.

1. stirringThe reaction mixture is stirred at it for 12 h
2. customdirectly purified by preparative LCMS