Water → 6-[5-amino-6-(4-methyl-thiazol-2-yl)-3-phenyl-2-pyrazinyl]-2-isopropyl-3(2H)-pyridazinone

Participants

Reaction Steps

A solution of 3-amino-6-(1-isopropyl-6-oxo-1,6-dihydro-3-pyridazinyl)-5-phenyl-2-pyrazinecarbothioamide (100 mg) and 1-chloroacetone (37.9 mg) in DMF (0.27 ml) was heated at 100-105° C. for 10 hours. After cooling, sat. aq. NaHCO3 solution (0.5 ml) and water (1 ml) were added to the mixture to yield a precipitate. The precipitate was collected by filtration, dissolved in CHCl3, dried over MgSO4 and concentrated under reduced pressure to give a residue. The residue was subjected to column chromatography on silica gel eluting with a mixture of n-hexane and EtOAc (60:40 v/v) to give 6-[5-amino-6-(4-methyl-thiazol-2-yl)-3-phenyl-2-pyrazinyl]-2-isopropyl-3(2H)-pyridazinone as a solid (58 mg).

Provenance & Evidence