Hydrochloric Acid → 2-[4-(4-{[2-Amino-6-(trifluoromethyl)pyrimidin-4-yl]amino}-2-fluorophenoxy)-1H-pyrrolo[2,3-b]pyridin-3-yl]ethanol

Participants

Reaction Steps

130 mg (0.45 mmol) of 2-[4-(4-amino-2-fluorophenoxy)-1H-pyrrolo[2,3-b]pyridin-3-yl]ethanol and 107 mg (0.54 mmol) of 4-chloro-6-(trifluoromethyl)pyrimidine-2-amine are suspended in 6 ml of water. 0.6 ml (0.6 mmol) of 1N hydrochloric acid is added and the mixture is heated at reflux overnight. Using 1N aqueous sodium hydroxide solution, the suspension is adjusted to pH 10, resulting in the precipitation of crystals. The crystals are filtered off with suction, washed with water and purified by column chromatography on silica gel (mobile phase: dichloromethane/methanol (7N ammonia) 100:1 to 100:3).

Provenance & Evidence