反应详情

10% Pd/C (100 mg) was added to a solution of trans(±)-3-(tert-butoxycarbonyl)amino-1-(diphenylmethyl)-2-ethylazetidine obtained in Example (234d) (530 mg, 1.45 mmol) in methanol (7 mL), and the mixture was stirred in a hydrogen stream at 40° C. for 13 hours. The reaction solution was filtered, and then the filtrate was concentrated under reduced pressure. A 1 N aqueous hydrochloric acid solution was added to the resulting residue. The aqueous layer was washed with ethyl acetate, and then saturated aqueous sodium bicarbonate solution was added, followed by extraction with ethyl acetate and a chloroform/methanol mixed solvent. The combined organic layers were dried over anhydrous magnesium sulfate and filtered. Thereafter, the filtrate was concentrated under reduced pressure to obtain 206 mg of the title compound as a white solid (71%).

1. filtrationThe reaction solution was filtered
2. concentrationthe filtrate was concentrated under reduced pressure
3. additionA 1 N aqueous hydrochloric acid solution was added to the resulting residue
4. washThe aqueous layer was washed with ethyl acetate
5. additionsaturated aqueous sodium bicarbonate solution was added
6. extractionfollowed by extraction with ethyl acetate
7. dry with materialThe combined organic layers were dried over anhydrous magnesium sulfate
8. filtrationfiltered
9. concentrationThereafter, the filtrate was concentrated under reduced pressure