反应详情

To a 100 mL round bottom flask was added ethyl 4-(5-formyl-2-furanyl)benzoate (100 mg, 0.41 mmol, commercially available), [2-(3-fluorophenyl)ethyl]amine (0.070 mL, 0.49 mmol), NaBH(OAc)3 (261 mg, 1.23 mmol) and DCE (10 mL). The reaction was stirred at room temperature overnight, quenched with H2O, and extracted with CH2Cl2 (×3). The organic layer was washed with brine, dried with MgSO4 and concentrated under reduced pressure to give 150 mg of ethyl 4-[5-({[2-(3-fluorophenyl)-ethyl]amino}methyl)-2-furanyl]benzoate (used without further purification). LC/MS (method A) 1.97 min; m/z 368 (M+H).

1. customquenched with H2O
2. extractionextracted with CH2Cl2 (×3)
3. washThe organic layer was washed with brine
4. dry with materialdried with MgSO4
5. concentrationconcentrated under reduced pressure