3-(tert-Butylaminosulphonyl)benzeneboronic acid → HCID 66710966, compound

Participants

Reaction Steps

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 (0.050 g, 0.00010 mol) and 3-t-Butylsulfamoylphenylboronic acid (0.028 g, 0.00011 mol) were reacted. Purification by prep plate chromatography gave N-tert-Butyl-3-(2-{2-methoxy-4-[4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-phenylamino}-pyrrolo[2,1-f][1,2,4]triazin-7-yl)-benzenesulfonamide as a tan solid (0.032 g, 51%). MP: 214-216° C.; 1H-NMR (DMSO-d6, 400 MHz) δ 8.96 (s, 1H), 8.54 (s, 1H), 8.35-8.34 (d, 1H), 7.80 (t, 1H), 7.78-7.77 (d, 1H, J=2.88 Hz), 7.66 (t, 1H), 7.58 (s, 1H), 7.20-7.19 (d, 1H, J=4.80 Hz), 6.97-6.96 (d, 1H, J=4.72 Hz), 6.66 (s, 1H), 6.62-6.60 (d, 1H), 3.83 (s, 3H), 3.73-3.70 (d, 2H), 2.70-2.63 (m, 2H), 2.38-2.25 (m, 4H), 2.14 (s, 3H), 1.89-1.81 (d, 2H), 1.60-1.45 (q, 2H).

Provenance & Evidence