反应详情

5-{4-[(1,1-dioxidothiomorpholin-4-yl)methyl]phenyl}-N-[3-(4-methylpiperazin-1-yl)phenyl][1,2,4]triazolo[1,5-a]pyridin-2-amine was prepared from 5-{4-[(1,1-dioxidothiomorpholin-4-yl)methyl]phenyl}[1,2,4]triazolo[1,5-a]pyridin-2-amine (75.0 mg, 0.210 mmol) and 1-(3-bromo-phenyl)-4-methyl-piperazine (65.0 mg, 0.255 mmol) with 2,2′-bis-dicyclohexylphosphanyl-biphenyl (22.0 mg, 0.0402 mmol) as the ligand in a manner analogous to Step 2d and was isolated as an off-white solid (0.052 g, 47%). MP=150-152° C. 1H NMR (400 MHz, CDCl3, δ, ppm): 8.02 (d, J=7.7 Hz, 2H), 7.55-7.42 (m, 5H), 7.17 (t, J=7.8 Hz, 1H), 6.97 (d, J=7.0 Hz, 1H), 6.87-6.80 (m, 2H), 6.55 (d, J=8.3 Hz, 1H), 3.76 (s, 2H), 3.24-3.19 (m, 4H), 3.14-3.03 (m, 8H), 2.58-2.53 (m, 4H), 2.36 (s, 3H). MS=532 (MH)+.