反应详情

To a cooled (−20° C.) solution of N-Boc-O-benzyl-D-serine (26 g) in tetrahydrofuran (208 mL), N-methylmorpholine (15 mL) was added and reaction mixture was stirred for 5 minutes. isobutylchloformate (18 mL) was added to the reaction mixture in 5 minutes at −20° C. The solution was further stirred for 5 minutes at −20° C. and benzyl amine (15.01 mL) was added to in it in 5 minutes at −20° C. The solution was stirred for 1 hr at −20° C. The solution was allowed to warm at room temperature and stirred for 1 hour. The precipitated hydrochloride salt of N-methylmorpholine was filtered. The filtrate was concentrated under vacuum to obtain solid 17 g N-benzyl-O-benzyl-N2-Boc-D-serinamide after crystallization from diisopropylether.

1. additionwas added
2. customreaction mixture
3. additionisobutylchloformate (18 mL) was added to the reaction mixture in 5 minutes at −20° C
4. stirringThe solution was further stirred for 5 minutes at −20° C.
5. stirringThe solution was stirred for 1 hr at −20° C
6. stirringstirred for 1 hour
7. filtrationThe precipitated hydrochloride salt of N-methylmorpholine was filtered
8. concentrationThe filtrate was concentrated under vacuum