反应详情

This was prepared by the method described in example 4 but using 4-chloro-6-methoxy-7-(3-morpholin-4-ylpropoxy)quinazoline (200 mg, 0.59 mmol), 5-chloro-7-(4-methoxypent-1-yn-1-yl)-1,3-benzodioxole-4-amine (174 mg, 0.65 mmol) and sodium bis(trimethylsilyl)amide (1.0M in THF, 1.24 ml) in DMF (3 ml). The crude product was purified by column chromatography on silica using increasing concentrations of methanol in dichloromethane as eluent. There was thus obtained the title compound (216 mg, 64%) as an off-white solid; NMR Spectrum:(CDCl3) 1.33 (d, 3H), 2.12 (quintet, 2H), 2.47 (m, 4H), 2.55 (m, 3H), 2.74 (dd, 1H), 3.40 (s, 3H), 3.58 (m, 1H), 3.71 (m, 4H), 3.98 (s, 3H), 4.25 (t, 2H), 6.07 (s, 2H), 6.90 (s, 1H), 7.03 (s, 1H), 7.09 (s, 1H), 7.30 (s, 1H ), 8.62 (s, 1H); Mass Spectrum: M+H+ 569/571.

1. customThis was prepared by the method
2. customThe crude product was purified by column chromatography on silica using
3. temperatureincreasing concentrations of methanol in dichloromethane as eluent