HCID 70655350, compound → HCID 73438245, 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-(4-fluorotetrahydro-2H-pyran-4-yl)phenyl)-5-fluoropicolinic acid (see US2012/225062) gave 206. 1H NMR (400 MHz, DMSO-d6) δ 10.22 (s, 1H), 8.30 (dd, J=8.7, 4.0 Hz, 1H), 8.17 (t, J=8.9 Hz, 1H), 7.92 (s, 1H), 7.41 (d, J=9.2 Hz, 2H), 4.81 (dd, J=10.3, 3.8 Hz, 1H), 4.17 (ddd, J=49.1, 5.9, 3.1 Hz, 1H), 4.02-3.96 (m, 1H), 3.96-3.84 (m, 3H), 3.75 (s, 3H), 3.74-3.64 (m, 2H), 3.09-2.99 (m, 1H), 2.33-2.13 (m, 2H), 2.10-1.99 (m, 1H), 1.93-1.80 (m, 2H), 1.80-1.52 (m, 5H). LCMS (ES+) m/z 566 (M+1).

Provenance & Evidence