反应详情

Following the procedure for Example 111 starting from tert-butyl ((3S,4R,7S)-3-fluoro-7-(1-methyl-4-nitro-1H-pyrazol-5-yl)oxepan-4-yl)carbamate (Intermediate 80), and replacing 5-((tert-butoxycarbonyl)amino)-2-(2,6-difluorophenyl)thiazole-4-carboxylic acid with 2-(2,6-difluorophenyl)thiazole-4-carboxylic acid (see US2012/225061) gave 321. 1H NMR (400 MHz, DMSO-d6) δ 9.94-9.85 (m, 1H), 8.63 (d, J=1.2 Hz, 1H), 7.81 (d, J=1.1 Hz, 1H), 7.69-7.60 (m, 1H), 7.33 (t, J=8.7 Hz, 2H), 4.81 (dd, J=10.9, 3.5 Hz, 1H), 4.44-4.24 (m, 1H), 4.23-4.10 (m, 1H), 3.99 (ddd, J=37.2, 14.8, 3.5 Hz, 1H), 3.77 (s, 3H), 2.11-2.02 (m, 1H), 1.90-1.76 (m, 1H), 1.75-1.63 (m, 2H). LCMS (ES+) m/z 452 (M+1).