1-Cyclohexyl-3-(2-morpholinoethyl)carbodiimide metho-p-toluenesulfonate → 5,6-Difluoro-2-(isopropylamino)-1H-benzimidazole

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Reaction Steps

4,5-Difluoro-1,2-phenylenediamine (2.87 g, 19.91 mmol), isopropyl isothiocyanate (2.19 g, 21.65 mmol), 1-cyclohexyl-3-(2-morpholinoethyl)carbodiimide metho-p-toluenesulfonate (11.38 g, 26.87 mmol) and pyridine (75 mL) were used according to general method I. The product was recrystallized from 1,4-dioxane to afford 2.23 g (53%) of a white solid; m.p. 188-189° C. Anal. Calcd for C10H11F2N3: C, 56.87; A, 5.25; N, 19.89. Found C, 56.95; H, 5.25; N, 19.98.

Provenance & Evidence