Phosphorus oxychloride → 5-Chloro-7-(2-chloro-4-fluorophenyl)-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 1.25 g (3.2 mmol) of 7-(2-chloro-4-fluorophenyl)-2-[1-(propan-2-yl)piperidin-4-yl][1,2,4]triazolo[1,5-c]pyrimidin-5(6H)-one (Example 50A), 1.46 g (6.41 mmol) of benzyltriethylammonium chloride were added and the reaction mixture was stirred at 120° C. for 16 h. The reaction mixture was concentrated and carefully, with vigorous stirring, added to ice. The mixture was stirred for another 10 min. Three times, the aqueous phase was extracted with dichloromethane. The combined organic phases were freed from the solvent and the residue was dried under high vacuum. This gave 715 mg (55% of theory) of the product.

Provenance & Evidence