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-fluoro-2-iodo-1,3-benzothiazole and conducting the Suzuki coupling at 50° C. for 1.5 h, the title compound was obtained as a yellow solid. 1H NMR (400 MHz, CD3OD): δ=8.84 (d, J=2.0 Hz, 1H), 8.41 (m, 1H), 8.40 (s, 1H), 8.09 (s, 1H), 8.04 (dd, J=0.8, 8.0 Hz, 1H), 7.66 (m, 1H), 7.38 (m, 1H), 4.66 (m, 1H), 3.62 (dt, J=3.2, 13.2, 2H), 3.24-3.28 (m, 2H), 2.36-2.40 (m, 4H). MS(ES+): m/z=395.12 [MH+]. HPLC: tR=1.62 min (polar—5 min, ZQ3).

1. customat 50° C.
2. customfor 1.5 h