反应详情

The title compound was prepared in an analogous fashion to that described in Example 41 using 5-bromo-6-(3-(hydroxymethyl)azetidin-1-yl)-N-(4-(trifluoromethoxy)phenyl)nicotinamide (Stage 39.1) and 3-methyl-1-(tetrahydro-2H-pyran-2-yl)-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole (Stage 41.1) to afford a beige lyophilizate. HPLC (Condition 7) tR=5.488 min, UPLC-MS (Condition 3) tR=0.89 min, m/z=448.1 [M+H]+; 1H-NMR (400 MHz, DMSO-d6) δ ppm 2.27 (s, 3H) 2.56-2.69 (m, 1H) 3.46 (d, J=6.26 Hz, 2H) 3.51-3.57 (m, 2H) 3.79 (t, J=8.6 Hz, 2H) 6.16 (s, 1H) 7.34 (d, J=8.60 Hz, 2H) 7.83-7.90 (m, J=9.00 Hz, 2H) 8.01 (d, J=2.35 Hz, 1H) 8.70 (d, J=2.35 Hz, 1H) 10.20 (br.s, 1H), 12.04 (br.s, 1H).

1. customto afford a beige lyophilizate