反应详情

To a mixture of 5-[5-(2,6-dichlorophenylmethanesulfonyl)-2-oxo-1,2-dihydro-indol-(3Z)-ylidenemethyl]-2,4-dimethyl-1H-pyrrole-3-carboxylic acid (100 mg, 0.2 mmol), EDAC (76 mg, 2 eq.), HOBt (27 mg, 1 eq.) in DMF (4 mL) was added triethyamine (0.08 mL, 0.57 mmol) and cyclopropyl-(R)-1-pyrrolidin-2-ylmethyl-amine (0.05 mL). After stirring at rt for 18 h, the reaction was basified with sodium bicarbonate, followed by extraction with 5% of methanol in dichloromethane. After concentration, the residue was purified on a silica gel column eluting with 5% of methanol in dichloromethane to give 80 mg (64%) of the titled compound.

1. extractionfollowed by extraction with 5% of methanol in dichloromethane
2. concentrationAfter concentration
3. customthe residue was purified on a silica gel column
4. washeluting with 5% of methanol in dichloromethane