反应详情

A solution of 82.0 g (0.31 mol) of 1-benzyl-3-(R)-hydroxymethyl-4-(S)-phenyl pyrrolidine (from EXAMPLE 1, Step C) and 46.5 g (0.36 mol) of DIEA in 1 L of CH2Cl2 was treated with 54.2 g (0.36 mol) of t-butyldimethylsilyl chloride and the resulting mixture was stirred at rt for 20 h. The reaction was quenched with 750 mL of sat'd NaHCO3 and the layers were separated. The organic layer was combined with 150 g of silica gel and aged for 45 min. The mixture was filtered and the filtrate was concentrated to afford 117 g (100%) of the title compound.

1. customThe reaction was quenched with 750 mL of sat'd NaHCO3
2. customthe layers were separated
3. waitThe organic layer was combined with 150 g of silica gel and aged for 45 min
4. filtrationThe mixture was filtered
5. concentrationthe filtrate was concentrated