反应详情

A solution of (2S)-2-((3S)-3-{[(6-chloro-2-naphthyl)sulfonyl]amino}-2-oxopyrrolidin-1-yl)propanoic acid (0.408 g) in DCM (21 ml) was treated with 1-[3-(dimethylamino)propyl]-3-ethylcarbodiimide hydrochloride (0.394 g), HOBT (0.278 g) and triethylamine (0.286 ml) and stirred at room temperature for 1 h. A solution of benzyl (3S)-piperidin-3-ylcarbamate (0.361 g) in DCM (1 ml) was then added and stirring continued for 72 h. The mixture was partitioned between DCM and water. The separated organic extracts were washed with water and brine, dried (over magnesium sulphate), and concentrated under reduced pressure. The residue was purified using Biotage™ chromatography (eluting with hexane:ethyl acetate 1:7→1:10) to give the title compound (0.268 g) as an oil.

1. stirringstirring
2. waitcontinued for 72 h
3. customThe mixture was partitioned between DCM and water
4. washThe separated organic extracts were washed with water and brine
5. dry with materialdried (over magnesium sulphate)
6. concentrationconcentrated under reduced pressure
7. customThe residue was purified
8. washBiotage™ chromatography (eluting with hexane:ethyl acetate 1:7→1:10)