反应详情

This was prepared using the method described in example 13 using N-[5-chloro-7-(3-methoxyprop-1-yn-1-yl)-1,3-benzodioxol-4-yl]-7-(3-chloropropoxy)-6-methoxyquinazolin-4-amine (250 mg, 0.51 mmol) and 1-methylpiperazin-2-one (290 mg, 2.54 mmol) in 2-methoxyethanol (4 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 (229 mg, 79%) as a pale brown solid; NMR Spectrum: ()MSOd6) 1.98 (quintet, 2H), 2.56 (t, 2H), 2.69 (t, 2H), 2.82 (s, 3H), 3.01 (s, 2H), 3.30 (t, 2H), 3.35 (s, 3H), 3.93 (s, 3H), 4.19 (t, 2H), 4.37 (s, 2H), 6.16 (s, 2H), 7.15 (s, 1H), 7.18 (s, 1H), 7.81 (s, 1H), 8.32 (s, 1H), 9.52 (s, 1H); Mass Spectrum: M+H+ 566/568.

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