反应详情

Following the procedure for Example 101 starting from tert-butyl ((3S,4R,7S)-7-(4-(2-bromothiazole-4-carboxamido)-1-methyl-1H-pyrazol-5-yl)-3-methoxyoxepan-4-yl)carbamate (Intermediate 102), and replacing 3,6-dihydro-2H-pyran-4-boronic acid pinacol ester with (2,6-difluorophenyl)boronic acid gave 347. 1H NMR (500 MHz, DMSO-d6) δ 10.13 (s, 1H), 8.65 (s, 1H), 7.94 (s, 1H), 7.69-7.65 (m, 1H), 7.40-7.36 (m, 2H), 5.11-5.09 (m, 1H), 3.85-3.79 (m, 2H), 3.72 (s, 3H), 3.57 (s, 2H), 3.46-3.43 (m, 1H), 3.30 (s, 1H), 3.01 (s, 3H), 2.43-2.37 (m, 1H), 1.74-1.58 (m, 3H). LCMS (ES+) m/z 464 (M+1).