反应详情

To a solution of benzyl (S)-1-((1S,2R,4R)-2-acetamido-4-(tert-butylamino)cyclohexyl)-2-oxopyrrolidin-3-ylcarbamate (43.3 g, 98 mmol) in methanol (400 ml), 10% wet Pd/C (4.34 g) was added. The mixture was evacuated and back-filled with hydrogen with a hydrogen balloon. The mixture was stirred at room temperature for 5 h. The mixture was filtered and washed with methanol (500 ml) and concentrated under vacuum to dryness. The crude product obtained was distilled with IPA (2×100 ml) under reduced pressure to give product N-((1R,2S,5R)-2-((S)-3-amino-2-oxopyrrolidin-1-yl)-5-(tert-butylamino)cyclohexyl)acetamide as an oil (30 g, 98% yield). This amine was used in the next step without further purification.

1. customThe mixture was evacuated
2. additionback-filled with hydrogen with a hydrogen balloon
3. filtrationThe mixture was filtered
4. washwashed with methanol (500 ml)
5. concentrationconcentrated under vacuum to dryness
6. customThe crude product obtained
7. distillationwas distilled with IPA (2×100 ml) under reduced pressure