反应详情

A solution of methanesulfonyl chloride (10 ml) in tetrahydrofuran (20 ml) was dropwise added to a solution of (2S,4R)-1-benzyloxycarbonyl-2-carboxymethyloxymethyl-4-hydroxypyrrolidine (19.95 g) and triethylamine (27 ml) in tetrahydrofuran (200 ml) at -10°~5° C. and the mixture was stirred at the same temperature for 1 hour The mixture was poured into water (200 ml), adjusted to pH 2.5 with 6N hydrochloric acid and extracted with ethyl acetate (150 ml×2). The organic layer was washed with brine (200 ml×2), dried over magnesium sulfate and concentrated under reduced pressure to give (2S,4R)-1-benzyloxycarbonyl-2-carboxymethyloxymethyl-4methanesulfonyloxypyrrolidine (24.85 g).

1. extractionextracted with ethyl acetate (150 ml×2)
2. washThe organic layer was washed with brine (200 ml×2)
3. dry with materialdried over magnesium sulfate
4. concentrationconcentrated under reduced pressure