HCID 70655525, compound → HCID 73425569, compound

Participants

Reaction Steps

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-(1-hydroxycyclopropyl)phenyl)-5-fluoropicolinic acid (see US2012/225062) gave 204. 1H NMR (400 MHz, DMSO-d6) δ 10.17 (s, 1H), 8.27 (dd, J=8.7, 4.0 Hz, 1H), 8.13 (t, J=8.9 Hz, 1H), 7.90 (s, 1H), 7.09 (d, J=9.8 Hz, 2H), 6.26 (s, 1H), 4.81 (dd, J=10.5, 3.7 Hz, 1H), 4.34-4.09 (m, 1H), 4.07-3.84 (m, 2H), 3.75 (s, 3H), 3.12-2.99 (m, 1H), 2.11-1.99 (m, 1H), 1.83-1.53 (m, 5H), 1.27-1.08 (m, 4H). LCMS (ES+) m/z 520 (M+1).

Provenance & Evidence