反应详情

To (2R)-3-hydroxy-1-methoxy-1-oxopropan-2-aminium chloride (1 eq.) in MeOH (1.3 M) at 0° C. was added triethylamine (1 eq.). The reaction mixture was stirred for 10 minutes and benzaldehyde (1 eq) was added. The reaction mixture was stirred for 2 hours and NaBH4 (1.5 eq.) was added portionwise to the reaction mixture over 30 min. The reaction mixture was stirred at rt for 5 hours and poured into a 1:1 mixture of saturated aqueous NH4Cl and EtOAc. The aqueous layer was extracted with EtOAc and the combined organic layers were washed with brine and water, dried over Na2SO4, filtered and concentrated. The crude product was used as such for the next step.

1. stirringThe reaction mixture was stirred for 2 hours
2. stirringThe reaction mixture was stirred at rt for 5 hours
3. extractionThe aqueous layer was extracted with EtOAc
4. washthe combined organic layers were washed with brine and water
5. dry with materialdried over Na2SO4
6. filtrationfiltered
7. concentrationconcentrated