反应详情

(S)-Benzyl 4-oxopyrrolidine-2-carboxylate hydrochloride (1.92 g, 8.8 mmol), the acid (in this case (S)-2-(methoxycarbonylamino)-3-methylbutanoic acid) (1.84 g, 10.56 mmol) and HATU (5.02 g, 13.2 mmol) were weighed out in a round bottom flask and dissolved in anhydrous DMF (44 mL). To this mixture was added DIPEA (6.82 g, 52.8 mmol) at room temperature and the mixture was stirred for 2 h. The crude mixture was diluted with EtOAc and washed respectively with brine, 10% Na2CO3 and brine again, and the mixture was dried over MgSO4, after filtration the mixture was concentrated down on rotovap. The residue was then purified on normal phase chromatography. (2.45 g, 74%).

1. washwashed respectively with brine, 10% Na2CO3 and brine again
2. dry with materialthe mixture was dried over MgSO4
3. filtrationafter filtration the mixture
4. concentrationwas concentrated down on rotovap
5. customThe residue was then purified on normal phase chromatography