反应详情

温度

122.5 °C

A mixture of 6-(5-amino-6-bromo-3-phenyl-2-pyrazinyl)-2-isopropyl-3(2H)-pyridazinone (150 mg) and N-(2-aminoethyl)acetamide (0.112 ml) in 1,2-dimethyl-2-imidazolidinone (0.3 ml) was heated at 120-125° C. for 50 hours. After addition of water (3 ml), an aqueous layer was removed by decantation to give a residue. The residue was dissolved in CHCl3, dried over MgSO4, concentrated under reduced pressure and purified by column chromatography on silica gel eluting with a mixture of MeOH and EtOAc (3:97 v/v) to give a solid. The solid was suspended in acetone to give N-(2-{[3-amino-6-(1-isopropyl-6-oxo-1,6-dihydro-3-pyridazinyl)-5-phenyl-2-pyrazinyl]amino}ethyl)acetamide (28 mg).

1. customan aqueous layer was removed by decantation
2. customto give a residue
3. dry with materialdried over MgSO4
4. concentrationconcentrated under reduced pressure
5. custompurified by column chromatography on silica gel eluting with a mixture of MeOH and EtOAc (3:97 v/v)
6. customto give a solid