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 6-(2,6-difluoro-4-(2-hydroxypropan-2-yl)phenyl)-5-fluoropicolinic acid (see US2012/225062) gave 200. 1H NMR (400 MHz, DMSO-d6) δ 10.20 (s, 1H), 8.28 (dd, J=8.7, 4.0 Hz, 1H), 8.14 (t, J=8.9 Hz, 1H), 7.89 (s, 1H), 7.34 (d, J=9.8 Hz, 2H), 5.36 (br, 1H), 4.80 (dd, J=10.4, 3.7 Hz, 1H), 4.37-4.06 (m, 1H), 4.02-3.87 (m, 2H), 3.75 (s, 3H), 3.13-3.00 (m, 1H), 2.10-1.99 (m, 1H), 1.85-1.57 (m, 3H), 1.47 (s, 6H). LCMS (ES+) m/z 522 (M+1).