反应详情

To a solution of 3-(4-(4-(3-fluorobenzyloxy)-3-chlorophenylamino)quinazolin-6-yl)prop-2-ynyl methanesulfonate (compound 10.2, 319 mg), DIPEA (0.37 mL) in dichloromethane (20 mL) at 0° C. was added 2-(dimethylphosphinoyl)ethanamine (83 mg) and the reaction mixture was stirred at room temperature overnight. The solvent was removed and the residue was purified by flash chromatography, eluting with 20% methanol in dichloromethane to give the desired product as yellow solid. LCMS ESI(+) m/z: 538 (M+1). 1H NMR (300 MHz, CDCl3) δ 9.47 (s, 1H), 8.87 (s, 1H), 8.70 (s, 1H), 7.95 (m, 2H), 7.85 (m, 2H), 7.62 (m, 2H), 7.38 (m, 1H), 6.98 (m, 1H), 5.10 (s, 2H), 4.25 (m, 2H), 3.87 (m, 1H), 3.58 (m, 1H), 2.05 (m, 2H), 1.57 (m, 6H).

1. customThe solvent was removed
2. customthe residue was purified by flash chromatography
3. washeluting with 20% methanol in dichloromethane