反应详情

To a solution of 0.33 g (1-amino-6-isoquinolinyl)carboxylic acid hydrochloride in 20 mL of N,N-dimethylformamide were added 0.34 g hydroxybenztriazole, 0.504 mL N-methylmorpholine, 0.525 g tert-butyl (S)-[[1-(2-amino-1-oxopropyl)piperidin-4-yl]oxy]acetic acid hydrochloride and 0.425 g 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide After stirring at room temperature for three days the mixture was concentrated. Dichloromethane and 1% aqueous sodium hydrogencarbonate were added to the residue and the organic layer was separated. The aqueous layer was washed four times with dichloromethane, the combined organic layers dried (sodium sulfate) and concentrated. The residue was purified by chromatography (silica gel, dichloromethane/methanol: 10/1 v/v followed by a purification using silica gel, ethyl acetate/methanol: 10/1 v/v) to give 0.619 g of the title compound.

1. concentrationwas concentrated
2. additionDichloromethane and 1% aqueous sodium hydrogencarbonate were added to the residue
3. customthe organic layer was separated
4. washThe aqueous layer was washed four times with dichloromethane
5. dry with materialthe combined organic layers dried (sodium sulfate)
6. concentrationconcentrated
7. customThe residue was purified by chromatography (silica gel, dichloromethane/methanol
8. custom10/1 v/v followed by a purification