Anisole → 5-Amino-7-chloro-2-(2-furyl)[1,2,4]triazolo[1,5-c]pyrimidine

Participants

Reaction Steps

Into 260 mL of trifluoroacetic acid, 50.0 g (130 mmol) of Compound D was dissolved, and 50 g (333 mmol) of trifluoromethanesulfonic acid and 42 mL (390 mmol) of anisole were added thereto, followed by stirring at room temperature for about 2 hours. After completion of the reaction, trifluoroacetic acid was evaporated under reduced pressure, and the residue was poured into ice-water. The mixture was adjusted to be alkaline with a 2 mol/L aqueous sodium hydroxide solution. The precipitated solid was washed with hexane and was reslurried with chloroform to obtain 25.6 g of Compound E as a white solid (yield: 83%).

Provenance & Evidence