Water → 5-Chloro-6-(trifluoromethyl)-1H-benzimidazol-2-amine

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Reaction Steps

318 mg (3 mmol) BrCN are dissolved in 0.6 ml acetonitrile and treated with 6 ml water. To this solution, 575 mg (2.73 mmol) 5-chloro-6-trifluoromethyl-benzene-1,2-diamine, dissolved in 6 ml methanol, are added dropwise within 30 min. After 2 hrs of stirring at room temperature, the reaction mixture is concentrated and the water solution extracted 2× with ethyl acetate. The combined organic phases where re-extracted 1× with water. The combined water phases where made alkaline (pH=8) with saturated NaHCO3-solution and extracted 2× with ethyl acetate. The combined organic phases where dried, filtered and evaporated.

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