反应详情

温度

25 °C

A mixture of 2-[2-cyclopentyl-1-(4-ethenesulfonyl-phenyl)-ethyl]-1H-pyrrolo[2,3-b]pyridine (prepared as in Example 92, 50 mg, 0.13 mmol) and morpholine (1.5 ml) was stirred at 25° C. for 20 min. Purification using a Waters automated flash system (column: Xterra 30 mm×100 mm, sample manager 2767, pump 2525, detector: ZQ mass and UV 2487, solvent system: acetonitrile and 0.1% ammonium hydroxide in water) afforded 2-{2-cyclopentyl-1-[4-(2-morpholin-4-yl-ethanesulfonyl)-phenyl]-ethyl}-1H-pyrrolo[2,3-b]pyridine (4 mg, 6%) as a white solid: LC/MS m/e calcd for C26H33N3O3S [M+H]+ 468.64, observed 468.1; 1H NMR (400 MHz, CD3OD) δ ppm 8.09 (d, J=4.3 Hz, 1H), 7.87-7.93 (m, 3H), 7.63 (d, J=8.3 Hz, 2H), 7.06 (dd, J=7.8, 5.1 Hz, 1H), 6.42 (s, 1H), 4.34 (t, J=8.0 Hz, 1H), 3.40-3.50 (m, 6H), 3.27-3.30 (m, 1H), 2.81 (t, J=6.4 Hz, 2H), 2.42 (br. s., 4H), 2.30 (dt, J=13.9, 7.2 Hz, 1H), 2.11-2.19 (m, 1H), 1.62-1.89 (m, 5H), 1.46-1.57 (m, 2H), 1.19-1.31 (m, 2H).

1. customPurification