反应详情

To a mixture of 4-(6-iodo-1H-indazol-1-yl)pyrimidin-2-amine (1-a1) (150 mg, 0.285 mmol) and piperidine (1 mL) was added tetrakis(triphenylphosphine)palladium (49.3 mg, 0.043 mmol), copper(I) iodide (8.1 mg, 0.043 mmol) and 2-(1,3-thiazol-2-yl)but-3-yn-2-ol (I-1) (131 mg, 0.854 mmol). The reaction was purged with N2 and stirred at RT for 30 min. The reaction mixture was concentrated in vacuo and the residue purified by reverse phase preparative HPLC to afford the title compound: 1H NMR (500 MHz, DMSO) δ 1.95 (3H, s), 7.04 (2H, br. s.), 7.08-7.13 (2H, m), 7.35 (1H, dd, J=8.20, 1.26 Hz), 7.70 (1H, d, J=3.15 Hz), 7.79 (1H, d, J=3.15 Hz), 7.89 (1H, d, J=8.51 Hz), 8.30 (1H, d, J=5.67 Hz), 8.50 (1H, s), 8.91 (1H, s). LC-MS: m/z=+363.4 (M+H)+.

1. customThe reaction was purged with N2
2. concentrationThe reaction mixture was concentrated in vacuo
3. customthe residue purified by reverse phase preparative HPLC