反应详情

To a solution of 3-(3-benzylureido)thiophene-2-carboxylic acid (Compound V-1) 49.7 mg (0.18 mmol) and N-hydroxybenzotriazol 6.1 mg (0.045 mmol) in dichloromethane 1 ml, 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide 43.1 mg (0.225 mmol) was added and the mixture was stirred at room temperature for 0.5 hr. A solution of (S)-2-amino-N-benzyl-N-(2,2-diethoxyethyl)propanamide (Compound VI-1) 44.2 mg (0.15 mmol) in dichloromethane 1 ml was added to the reaction mixture and the mixture was stirred at room temperature for 18 hrs. The reaction mixture was washed with sat. NaHCO3 aq. 1 ml, water 1 ml and brine 1 ml. The organic phase was filtered on celite 1 g and magnesium sulfate 150 mg. The mother solution was concentrated in vacuo and the residue was purified with PTLC (development solvent: chloroform:methanol=98:2) to obtain the titled compound 44.7 mg (54%).

1. stirringthe mixture was stirred at room temperature for 18 hrs
2. washThe reaction mixture was washed with sat. NaHCO3 aq. 1 ml, water 1 ml and brine 1 ml
3. filtrationThe organic phase was filtered on celite 1 g and magnesium sulfate 150 mg
4. concentrationThe mother solution was concentrated in vacuo
5. customthe residue was purified with PTLC (development solvent: chloroform:methanol=98:2)