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 2-iodo-5-methyl-1,3-benzothiazole and conducting the Suzuki coupling at 80° C. for 3 h, the title compound was obtained as a yellow solid. 1H NMR (400 MHz, DMSO-d6): δ=8.96-8.87 (brm, 1H), 8.75-8.65 (brm, 1H), 8.51 (d, J=2.0 Hz, 1H), 8.40 (s, 1H), 8.37 (brs, 1H), 8.35 (very brs, 1H), 8.06 (d, J=8.0 Hz, 1H), 8.06 (s, 1H), 7.36 (dd, J=8.0, 1.0 Hz, 1H), 4.56-4.48 (mc, 1H), 3.11 (brq, J=11.0 Hz, 2H), 2.30-2.10 (m, 4H); CH3 and additional 2H hidden under water peak. MS(ES+): m/z=391.14 (72) [MH+], 308.09 (100) [MH+-piperidine]. HPLC: tR=2.10 min (polar—5 min, ZQ2).

1. customat 80° C.
2. customfor 3 h