5-Amino-3-(1-methylpyrrol-2-yl)-1,2-benzisothiazole → 3-[3-(1-Methylpyrrol-2-yl)-1,2-benzisothiazol-5-yl]-6-(trifluoromethyl)uracil

Participants

Reaction Steps

To a mixture of 5-amino-3-(1-methylpyrrol-2-yl)-1,2-benzisothiazole(1.05 g, 4.59 mmol) and acetic acid is added 2-(dimethylamino)-4-(trifluoromethyl)-5H-1,3-oxazin-6-one (0.960 g, 4.60 mmol). The resultant mixture is stirred at reflux for two hours, cooled to room temperature, diluted with ice water and stirred vigorously for approximately 15 minutes. Filtration and drying affords the title compound as a gray solid (1.50 g, 83.3%, mp 125-130° C.) which is identified by NMR spectral analysis.

Provenance & Evidence