反应详情

To the 2-{(2R)-1-[(4-fluorophenyl)sulfonyl]aziridin-2-yl}ethanol from Step 3 dissolved in THF (0.2 M) was added TBSCl (1.1 equiv.) followed by imidazole (2.2 equiv.). The reaction mixture was stirred 1 h at rt, then filtered with washing of the solids with MTBE. The combined organics were washed (2×) with 1M HCl, brine (2×), dried over MgSO4, filtered and concentrated in vacuo. The residue was purified by column chromatography eluting with EtOAc/Hex (1:9) to give the title compound (85%) as a white solid.

1. filtrationfiltered
2. washwith washing of the solids with MTBE
3. washThe combined organics were washed (2×) with 1M HCl, brine (2×)
4. dry with materialdried over MgSO4
5. filtrationfiltered
6. concentrationconcentrated in vacuo
7. customThe residue was purified by column chromatography
8. washeluting with EtOAc/Hex (1:9)