反应详情

To a solution of 1-Boc-3-aminoazetidine 1a (1.0 g, 5.8 mmol) and methyl 2-formylbenzoate 2a (0.95 g, 5.8 mmol) in 1,2-dichloroethane (30 mL) and acetic acid (1.5 mL) was added Na(OAc)3BH (1.29 g, 6.08 mmol) at room temperature. The reaction was stirred for 5.5 h. It was quenched with aq. NaHCO3, and the resulting mixture was extracted with CH2Cl2. The organic solution was dried over Na2SO4 and concentrated. Purification by flash column chromatography (silica gel, 40% EtOAc/heptane) gave compound 2b (1.46 g).

1. customIt was quenched with aq. NaHCO3
2. extractionthe resulting mixture was extracted with CH2Cl2
3. dry with materialThe organic solution was dried over Na2SO4
4. concentrationconcentrated
5. customPurification by flash column chromatography (silica gel, 40% EtOAc/heptane)