[1-Methyl-3-(trifluoromethyl)-1H-pyrazol-4-yl]boronic acid → HCID 86713907, compound

Participants

Reaction Steps

Following the procedure for Example 101 starting from tert-butyl ((3R,4R,7S)-7-(4-(2-bromothiazole-4-carboxamido)-1-methyl-1H-pyrazol-5-yl)-3-fluorooxepan-4-yl)carbamate (Intermediate 100), and replacing 3,6-dihydro-2H-pyran-4-boronic acid pinacol ester with (1-methyl-3-(trifluoromethyl)-1H-pyrazol-4-yl)boronic acid gave 252. 1H NMR (400 MHz, DMSO-d6) δ 9.64 (s, 1H), 8.63 (s, 1H), 8.42 (s, 1H), 7.88 (s, 1H), 4.98-4.72 (m, 2H), 4.22-4.03 (m, 1H), 4.00 (s, 3H), 3.97-3.88 (m, 1H), 3.75 (s, 3H), 3.30-3.17 (m, 1H), 2.14-2.03 (m, 1H), 1.92-1.68 (m, 3H), 1.66-1.57 (m, 1H). LCMS (ES+) m/z 488 (M+1).

Provenance & Evidence