反应详情

The title compound (70 mg, 27%) was prepared as a white solid from (4-{[(2-hydroxyethyl)amino]sulfonyl}phenyl)boronic acid (130 mg, 0.55 mmol), 1-methylethyl 4-{[(6-bromo-3-pyridinyl)oxy]methyl}-1-piperidinecarboxylate (prepared as in Example 81, Step 1, 197 mg, 0.55 mmol), Pd(PPh3)2Cl2 (100 mg, 0.14 mmol), 2M Na2CO3 (2 mL) and DME (4 mL) in a manner similar to Example 21, Step 3. 1H NMR (400 MHz, CDCl3): δ 8.36 (d, 1H, J=2.9 Hz), 8.05 (d, 2H, J=8.6 Hz), 7.91 (d, 2H, J=8.6 Hz), 7.69 (d, 1H, J=8.8 Hz), 7.26 (dd, 1H, Ja=8.8 Hz, Jb=2.9 Hz), 5.11 (t, 1H, J=6.0 Hz), 4.96-4.83 (m, 1H), 4.20 (bs, 2H), 3.89 (d, 2H, J=6.2 Hz), 3.70-3.61 (m, 2H), 3.13-2.99 (m, 2H), 2.83-2.70 (m, 2H), 2.07-1.92 (m, 1H), 1.89-1.79 (m, 2H), 1.70 (bs, 1H), 1.37-1.17 (m, 8H); LRMS (ESI), m/z 478 (M+H).