1-methyl-5-(tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole → (R)-N-(4-(Chlorodifluoromethoxy)phenyl)-6-(3-hydroxypyrrolidin-1-yl)-5-(1-methyl-1H-pyrazol-5-yl)nicotinamide

関与物質

反応手順

The title compound was prepared in an analogous fashion to that described in Stage 2.1 using (R)-5-bromo-N-(4-(chlorodifluoromethoxy)phenyl)-6-(3-hydroxypyrrolidin-1-yl)nicotinamide (Stage 9.2) and 1-methyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole to afford a white powder. HPLC (Condition 4) tR=5.25 min, UPLC-MS (Condition 3) tR0.98 min, m/z=464.1 [M+H]+; 1H-NMR (400 MHz, DMSO-d6) δ ppm 1.65-1.89 (m, 2H) 2.87-3.00 (m, 1H) 3.09-3.29 (m, 3H) 3.59 (s, 3H) 4.19 (br. s, 1H) 4.87 (d, J=3.13 Hz, 1H) 6.39 (s, 1H) 7.27-7.36 (m, 2H) 7.50 (dd, J=1.76, 0.98 Hz, 1H) 7.78-7.88 (m, 2H) 8.00 (d, J=2.35 Hz, 1H) 8.78 (dd, J=2.35, 1.17 Hz, 1H) 10.15 (s, 1H).

情報源と証拠