反应详情

To a solution of 5-(6-(benzyloxymethyl)pyrimidin-4-yloxy)-1H-indole (0.8 g, 2.41 mmol) in 35 mL of DCE, CDI (1.17 g, 7.24 mmol) is added followed by TEA (1 mL, 7.24 mmol). Mixture is stirred at rt overnight and then 4-methoxy-3-(trifluoromethyl)aniline (1.38 g, 7.24 mmol) is added followed by stirring for 4 days. The reaction is diluted with DCM, washed with saturated aqueous NaHCO3 (×2), brine, and the organic layer is dried over Na2SO4. After concentration, the residue is purified by FCC (5-60% EtOAc/heptane) to give the title compound. MS (ESI) m/z 549.1 (M+1).

1. stirringby stirring for 4 days
2. washwashed with saturated aqueous NaHCO3 (×2), brine
3. dry with materialthe organic layer is dried over Na2SO4
4. concentrationAfter concentration
5. customthe residue is purified by FCC (5-60% EtOAc/heptane)