反应详情

The title compound was prepared in an analogous fashion to that described in Example 15 using (R)-5-bromo-6-(3-hydroxy-3-methylpyrrolidin-1-yl)-N-(4-(trifluoromethoxy)phenyl)nicotinamide (Stage 14.1) and (1H-pyrazol-3-yl)boronic acid to afford a white solid. HPLC Chiral (CHIRALCEL® OD-H, 250×4.6 mm, eluent: n-heptane/EtOH/MeOH (80:12:8), 1 mL/min, UV 210 nm) tR=5.49 min, UPLC-MS (Condition 3) tR=0.93 min, m/z=448.3 [M+H]+, m/z=446.1 [M−H]−, 492.1 [M+formic acid-H]−; 1H-NMR (400 MHz, DMSO-d6) δ ppm 1.20 (s, 3H) 1.65-1.81 (m, 2H) 2.99 (d, J=10.54 Hz, 1H) 3.06 (d, J=11.80 Hz, 1H) 3.24-3.33 (m, 1H) 3.48 (td, J=10.20, 7.22 Hz, 1H) 4.68 (s, 1H) 6.38 (d, J=2.01 Hz, 1H) 7.33 (d, J=9.16 Hz, 2H) 7.75 (br. s, 1H) 7.83-7.90 (m, 2H) 8.03 (d, J=2.51 Hz, 1H) 8.73 (d, J=2.38 Hz, 1H) 10.19 (br. s, 1H) 12.96 (br. s, 1H).

1. customto afford a white solid