反应详情

The title compound (11 mg, 25%) was prepared as a tan solid from {4-[(methylsulfonyl)amino]phenyl}boronic acid (22 mg, 0.1 mmol), 1-methylethyl 4-{[(4-bromophenyl)oxy]methyl}-1-piperidinecarboxylate (prepared as in Example 9, Step 2, 36 mg, 0.1 mmol), Pd(PPh3)2Cl2 (25 mg, 0.04 mmol), 2M Na2CO3 (1 mL) and DME (1 mL) in a manner similar to Example 21, Step 3, and worked up in a manner similar to Example 9, Step 3. 1H NMR (400 MHz, CDCl3): δ 7.55-7.45 (m, 4H), 7.30-7.20 (m, 2H), 6.95 (d, 2H, J=8.6 Hz), 6.38 (s, 1H), 4.99-4.83 (m, 1H), 3.84 (d, 2 H, J=6.4 Hz), 3.03 (s, 3H), 2.84-2.74 (m, 2H), 2.05-1.94 (m, 1H), 1.90-1.80 (m, 2H), 1.37-1.18 (m, 10H); LRMS (ESI), m/z 447 (M+H).