反应详情

To a cooled (−20° C.) solution of N-Boc-O-benzyl-D-serine (1 g) in dichloro methane (12 mL), triethylamine (0.44 mL) was added and stirred for 5 minutes and subsequently isobutylchloformate (0.51 mL) was added to the reaction mixture in 5 minutes at −20° C. The solution was stirred for 5 minutes at −20° C. and benzyl amine (0.44 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 to room temperature and stirred for 1 hour. The hydrochloride salt of N-methylmorpholine was filtered. Organic layer was concentrated under vacuum to obtain solid, 0.53 g N-benzyl-O-benzyl-N2-Boc-D-serinamide after crystallization by diisopropylether.

1. additionwas added
2. additionsubsequently isobutylchloformate (0.51 mL) was added to the reaction mixture in 5 minutes at −20° C
3. stirringThe solution was stirred for 5 minutes at −20° C.
4. stirringThe solution was stirred for 1 hr at −20° C
5. stirringstirred for 1 hour
6. filtrationThe hydrochloride salt of N-methylmorpholine was filtered
7. concentrationOrganic layer was concentrated under vacuum