(R)-5-Bromo-N-(4-(chlorodifluoromethoxy)phenyl)-6-(3-hydroxypyrrolidin-1-yl)nicotinamide → (R)-N-(4-(Chlorodifluoromethoxy)phenyl)-5-(5-cyano-1H-pyrrol-2-yl)-6-(3-hydroxypyrrolidin-1-yl)nicotinamide

関与物質

反応手順

The title compound was prepared in an analogous fashion to that described in Example 29 using (R)-5-bromo-N-(4-(chlorodifluoromethoxy)phenyl)-6-(3-hydroxypyrrolidin-1-yl)nicotinamide (Stage 22.1) and (1-(tert-butoxycarbonyl)-5-cyano-1H-pyrrol-2-yl)boronic acid (Stage 29.1) to afford a beige solid. UPLC-MS (Condition 3) tR=1.06 min, m/z=474.1 [M+H]+, m/z=472.2 [M−H]−; 1H NMR (400 MHz, DMSO-d6) δ ppm 1.69-1.81 (m, 1H) 1.81-1.91 (m, 1H) 2.94 (d, J=11.74 Hz, 1H) 3.22-3.28 (m, 1H) 3.32 (d, J=3.42 Hz, 1H) 3.40-3.49 (m, 1H) 4.23 (br. s, 1H) 4.88 (br. s, 1H) 6.30 (d, J=3.67 Hz, 1H) 7.00 (d, J=3.67 Hz, 1H) 7.33 (d, J=9.05 Hz, 2H) 7.82-7.89 (m, 2H) 8.07 (d, J=2.20 Hz, 1H) 8.76 (d, J=2.20 Hz, 1H) 10.17 (s, 1H) 12.60 (br. s, 1H).

情報源と証拠