Phosphorus oxychloride → 5-Chloro-7-(2,4-difluorophenyl)-2-[1-(propan-2-yl)piperidin-4-yl][1,2,4]triazolo[1,5-c]pyrimidine hydrochloride

Participants

Reaction Conditions

Reaction Steps

4.5 ml of phosphoryl chloride were added to 670 mg (1.72 mmol) of 7-(2,4-difluorophenyl)-2-[1-(propan-2-yl)piperidin-4-yl][1,2,4]triazolo[1,5-c]pyrimidin-5(6H)-one (Example 51A), 785 mg (3.45 mmol) of benzyltriethylammonium chloride were added and the reaction mixture was stirred at 120° C. for 7 h. The reaction mixture was concentrated and carefully, with vigorous stirring, added to ice. Three times, the aqueous phase was extracted with dichloromethane. The combined organic phases were freed from the solvent and used without further purification. This gave 590 mg (80% of theory) of the product.

Provenance & Evidence