Methanol → Methyl 2-Amino-4-(trifluoromethyl)benzoate

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Reaction Steps

2-Amino-4-trifluoromethyl-benzoic acid (141.2 g.), methanol (1.51 liters) and boron trifluoride etherate (506 cc.) are heated to the reflux temperature for 99 hours. The solution obtained is added to sodium carbonate (350 g.) in iced water (2.8 kg.). The mixture is stirred for 15 minutes and is then extracted with ethyl ether (3 liters). The ether layer is washed with water (250 cc.) and then dried over anhydrous magnesium sulphate (30 g.). After filtration and concentration, methyl 2-amino-4-trifluoromethyl-benzoate (137 g.) melting at 64° C is obtained.

Provenance & Evidence