反应详情

To a solution of tert-butyl 3-hydroxyazetidine-1-carboxylate (167 mg, 0.965 mmol) in THF (2 mL) was added sodium tert-butoxide (93 mg, 0.965 mmol). The reaction was stirred at room temperature for 20 min. The reaction was cooled to 0° C. and a solution of Example 95A (200 mg, 0.483 mmol) in THF (1 mL) was added. The reaction was stirred at 0-5° C. for 2 h. The reaction mixture was diluted with H2O and extracted with EtOAc (2×). The organic layer was combined and dried over MgSO4, filtered and concentrated to afford the title compound 260 mg (93%). MS (DCI/NH3) m/z 568 (M+H)+.

1. temperatureThe reaction was cooled to 0° C.
2. stirringThe reaction was stirred at 0-5° C. for 2 h
3. extractionextracted with EtOAc (2×)
4. dry with materialdried over MgSO4
5. filtrationfiltered
6. concentrationconcentrated