Ammonium formate → Methyl 2,3-diamino-4-(trifluoromethyl)benzoate

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Reaction Steps

To a stirring solution of methyl 2-amino-3-nitro-4-(trifluoromethyl)benzoate (5.80 g, 0.022 mol), ammonium formate (30.0 g, 0.476 mol) in ethanol (300 ml) was added 10% palladium on carbon (500 mg) at room temperature and stirred for 2 h. Insoluble was filtered off and filtrates were concentrated in vacuo. The residue was diluted with water and extracted with ethyl acetate. The extracts were washed with water, dried over magnesium sulfate and concentrated in vacuo. The residue was purified by column chromatography on silica gel with a 20% ethyl acetate/n-hexane to give 5.10 g (0.022 mol, 99%) of the title compound as a yellow powder.

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