2-(Methoxymethyl)benzeneboronic acid → [7-(2-Methoxymethyl-phenyl)-pyrrolo[2,1-f][1,2,4]triazin-2-yl]-{2-methoxy-4-[4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-phenyl}-amine

참여 물질

반응 단계

Following the procedure of example 532 (D), (7-Bromo-pyrrolo[2,1-f][1,2,4]triazin-2-yl)-{2-methoxy-4-[4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-phenyl}-amine (0.062 g, 0.00012 mol) and 2-Methoxymethyl phenylboronic acid (0.0226 g, 0.000132 mol) were reacted. Purification by prep plate chromatography gave [7-(2-Methoxymethyl-phenyl)-pyrrolo[2,1-f][1,2,4]triazin-2-yl]-{2-methoxy-4-[4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-phenyl}-amine (0.034 g, 51%) as a tan solid MP: 96-101 C; 1H-NMR (DMSO-d6, 400 MHz) δ 8.92 (s, 1H), 7.65-7.62 (m, 2H), 7.55 (m, 2H), 7.47-7.45 (t, 2H, J=3.56 Hz), 6.94-6.87 (q, 2H, J=4.56 Hz), 6.61-6.60 (d, 1H, J=2.28 Hz), 6.42-6.38 (d, 1H), 6.30-6.27 (d, 1H), 4.33 (s, 2H), 3.81 (s, 3H), 3.64-3.61 (d, 2H) 3.17 (s, 3H), 2.67-2.57 (m, 6H), 2.33 (br, 5H), 2.16 (s, 3H), 1.84-1.81 (m, 2H), 1.50-1.48 (m, 2H), 1.23-1.17 (br, 3H).

출처 및 근거