反应详情

Following the procedure for Example 101 starting from tert-butyl N-[2-bromo-4-[[5-[(2S,5R,6S)-5-(tert-butoxycarbonylamino)-6-fluoro-oxepan-2-yl]-1-methyl-pyrazol-4-yl]carbamoyl]thiazol-5-yl]carbamate (Intermediate 95), and replacing 3,6-dihydro-2H-pyran-4-boronic acid pinacol ester with (2,3,6-trifluorophenyl)boronic acid gave 332. 1H NMR (400 MHz, DMSO-d6) δ 9.32 (s, 1H), 7.81 (s, 1H), 7.63-7.51 (m, 3H), 7.31-7.23 (m, 1H), 4.79 (dd, J=10.7, 3.5 Hz, 1H), 4.46-4.29 (m, 2H), 4.24-4.11 (m, 1H), 4.09-3.92 (m, 1H), 3.75 (s, 3H), 2.08-2.00 (m, 1H), 1.84-1.75 (m, 1H), 1.74-1.66 (m, 2H). LCMS (ES+) m/z 485 (M+1).