反应详情

温度

40 °C

To a solution of N-(4-(3-fluorobenzyloxy)-3-chlorophenyl)-6-iodoquinazolin-4-amine (1.52 g), trimethyl(prop-2-ynyloxy)silane (0.7 mL), triethyl amine (0.5 mL) in DMF (10 mL) was added Pd(PPh3)2Cl2 (106 mg), CuI (114 mg) and the mixture was heated at 40° C. overnight. The solvent was removed, then methanol (10 mL) and 4N HCl (2 mL) were added. The reaction mixture was stirred at room temperature for one hour and the solvent was removed. Another 10 mL methanol and triethyl amine (2 mL) were added and the reaction mixture was stirred at room temperature for one hour. The solvent was removed and the residue was purified by flash chromatography, eluting with EtOAc to give the desired product. LCMS ESI(+) m/z: 434 (M+1). Yield: 86%.

1. customThe solvent was removed
2. additionmethanol (10 mL) and 4N HCl (2 mL) were added
3. customthe solvent was removed
4. additionAnother 10 mL methanol and triethyl amine (2 mL) were added
5. stirringthe reaction mixture was stirred at room temperature for one hour
6. customThe solvent was removed
7. customthe residue was purified by flash chromatography
8. washeluting with EtOAc