反应详情

2-(2-(benzylcarbamoyl)-1-methylhydrazinyl)acetic acid VI-3) 115 mg (0.49 mmol) and NMM (N-methylmorpholine) 0.33 ml were added in DMF 1.5 ml. Then, HOBt (hydroxybenzotriazole) 88 mg (0.65 mmol) and EDCI (N-(3-Dimethylaminopropyl)-N′-ethylcarbodiimide hydrochloride) 125 mg (0.65 mmol) were added and stirred at room temperature for 10 min. Compound (S)-2-amino-N-benzyl-N—((S)-1,1-diethoxypropan-2-yl)propanamide (IV-10) 100 mg (0.32 mmol) in DCM 1.5 ml and DMAP 4.1 mg (0.03 mmol) were added. The mixture was stirred overnight at room temperature. The mixture was diluted with EA 30 ml and washed with 10% citric acid 15 ml, sat. NaHCO3 15 ml and brine 15 ml. The solvent was removed in vacuum to give crude product, which was used directly in the next step.

1. stirringThe mixture was stirred overnight at room temperature
2. washwashed with 10% citric acid 15 ml, sat. NaHCO3 15 ml and brine 15 ml
3. customThe solvent was removed in vacuum
4. customto give crude product, which