反应详情

To a solution of 1,1-dimethylethyl 3-(aminomethyl)-4-hydroxy-1-pyrrolidinecarboxylate (3 g, 13.9 mmol) [Prepared according to Hong, C.-Y. J. Med. Chem. 1997, 40, 3584.] in DCM (100 mL) at 0° C. was added N-(benzyloxycarbonyloxy)succinimide (3.8 g, 15.3 mmol) portion-wise. After 1 h, the reaction was partitioned between H O-DCM. The aqueous phase was extracted several times with DCM and the combined organic fractions were dried (Na SO), concentrated and purified by column chromatography (silica, 3% MeOH in DCM (1% NH OH)) yielding the title compound (4.8 g, quant.) as a clear oil: LCMS (ES) m/e 351 (M+H).

1. customthe reaction was partitioned between H O-DCM
2. extractionThe aqueous phase was extracted several times with DCM
3. customthe combined organic fractions were dried (Na SO)
4. concentrationconcentrated
5. custompurified by column chromatography (silica, 3% MeOH in DCM (1% NH OH))