(5-Fluoropyridin-3-yl)boronic acid → HCID 73437702, compound

Participants

Reaction Steps

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-fluorooxepan-4-yl)carbamate (Intermediate 99), and replacing 3,6-dihydro-2H-pyran-4-boronic acid pinacol ester with (5-fluoropyridin-3-yl)boronic acid gave 239. 1H NMR (400 MHz, DMSO-d6) δ 9.87 (s, 1H), 9.15 (t, J=1.7 Hz, 1H), 8.74 (d, J=2.7 Hz, 1H), 8.55 (s, 1H), 8.37 (dt, J=9.5, 2.3 Hz, 1H), 7.84 (s, 1H), 4.87 (dd, J=10.5, 3.9 Hz, 1H), 4.58-4.36 (m, 1H), 4.34-4.20 (m, 1H), 4.16-3.92 (m, 1H), 3.79 (s, 3H), 3.37-3.23 (m, 2H), 2.15-2.05 (m, 1H), 1.91-1.67 (m, 5H). LCMS (ES+) m/z 435 (M+1).

Provenance & Evidence