反应详情

Following the procedure for 3-(7-fluoro-4-trifluoromethylbenzothiazol-2-yl)-5-(1-piperidin-4-yl-1H-pyrazol-4-yl)-pyridin-2-ylamine, using 7-bromo-2-iodo-1,3-benzothiazole and conducting the Suzuki coupling at 60° C. for 4 h, the title compound was obtained as a yellow solid. 1H NMR (400 MHz, DMSO-d6): δ=9.20-9.09 (brm, 1H), 9.02-8.90 (brm, 1H), 8.61 (very brs, 1H), 8.60 (s, 2H), 8.52 (s, 1H), 8.18 (d, J=8.0 Hz, 1H), 8.13 (s, 1H), 7.78 (d, J=8.0 Hz, 1H), 7.58 (t, J=8.0 Hz, 1H), 4.57-4.47 (mc, 1H), 3.40 (brd, J=12.8 Hz, 2H), 3.11 (brq, J=11.2 Hz, 2H), 2.31-2.12 (m, 4H). MS(ES+): m/z=454.98/457.00 (79/83) [MH+], 371.94/373.95 (95/100) [MH+-piperidine]. HPLC: tR=2.22 min (polar—5 min, ZQ2).

1. customat 60° C.
2. customfor 4 h