反应详情

温度

90 °C

A mixture of 6-oxa-3-aza-bicyclo[3.1.0]hexane-3-carboxylic acid tert-butyl ester (5.4 mmol, from Example 316) and triethylamine trihydrofluoride (5.4 mmol) was heated at 90° C. for 2 h, then cooled to rt. Aq. Na2CO3 was added and the mixture was extracted with EtOAc. The organic phase was dried (Na2SO4), concentrated and purified by silica gel chromatography (0-40% EtOAc in heptane) to afford (trans)-3-fluoro-4-hydroxypyrrolidine-1-carboxylic acid tert-butyl ester as a colorless oil.

1. temperaturecooled to rt
2. extractionthe mixture was extracted with EtOAc
3. dry with materialThe organic phase was dried (Na2SO4)
4. concentrationconcentrated
5. custompurified by silica gel chromatography (0-40% EtOAc in heptane)