Phosphorus oxychloride → 5-Chloro-7-(2,4-dichlorophenyl)-2-(1-methylpiperidin-4-yl)[1,2,4]triazolo[1,5-c]pyrimidine

Participants

Reaction Conditions

Reaction Steps

270 mg (0.71 mmol) of 7-(2,4-dichlorophenyl)-2-(1-methylpiperidin-4-yl)[1,2,4]triazolo[1,5-c]pyrimidin-5(6H)-one (Example 48A) were initially charged in phosphorus oxychloride (2 ml), 650 mg (2.90 mmol) of benzyltriethylammonium chloride were added and the mixture was then stirred at 120° C. for 3 h. The reaction mixture was poured into saturated aqueous sodium bicarbonate solution (150 ml), and solid sodium bicarbonate was added until a pH of 7 had been reached. The solid was filtered off with suction and dried. This gave 190 mg (65% of theory) of the product as a solid.

Provenance & Evidence