反应详情

To a solution of (2S,3S,4S,5R,6S)-3,4,5-tribenzyloxy-6-[4-chloro-3-[(2,3-difluoro-4-methoxy-phenyl)methyl]phenyl]-6-methoxy-tetrahydropyran-2-carbaldehyde 21l (0.52 g, 0.68 mmol) in N,N-dimethyl formamide (20 mL) were added 1,8-diazabicyclo[5.4.0]undec-7-ene (0.05 mL, 0.34 mmol) and formaldehyde (0.83 mL, 10.28 mmol, 37 wt % solution) in turn at room temperature. The mixture was stirred at room temperature for 16 hours, and then ethyl acetate (50 mL) was added. The resulting mixture was washed with water (60 mL×5), dried over anhydrous sodium sulfate and filtered. The filtrate was concentrated in vacuo to give the title compound 21m as yellow oil (0.52 g, 100%). This material was not further purified.

1. washThe resulting mixture was washed with water (60 mL×5)
2. dry with materialdried over anhydrous sodium sulfate
3. filtrationfiltered
4. concentrationThe filtrate was concentrated in vacuo