反应详情

温度

40 °C

A solution of 4-methyl-[2,2′]bipyrimidinyl-5-carboxylic acid (184 mg, 0.85 mmol) and 2-cyclopropyl-5-fluoro-indol-1-ylamine (135 mg, 0.71 mmol) in DMF (3 mL) is stirred at 40° C. for 1 h. The mixture is treated with DMTMM (235 mg, 0.71 mmol) and stirred at 40° C. for 1 h. The mixture is diluted with saturated aqueous Na2CO3 (5 mL) and stirred for 5 min. The precipitate is collected by filtration and dried in vacuo to afford 4-methyl-[2,2′]bipyrimidinyl-5-carboxylic acid (2-cyclopropyl-5-fluoro-indol-1-yl)-amide (35 mg, 13%). MS: 389 (M+H); 1H NMR (300 MHz, DMSO-d6): δ 11.93 (s, NH, 1H), 9.31 (s, 1H), 9.06 (d, 2H), 7.70 (m, 1H), 7.42 (m, 1H), 7.26 (m, 1H), 6.97 (m, 1H), 6.16 (s, 1H), 2.79 (s, 3H), 1.97 (m, 1H), 1.01 (m, 2H), 0.74 (m, 2H).

1. stirringstirred for 5 min
2. filtrationThe precipitate is collected by filtration
3. customdried in vacuo