Phosphorus oxychloride → 5-Chloro-7-[4-(trifluoromethyl)phenyl][1,2,4]triazolo[1,5-c]pyrimidine

Participants

Reaction Conditions

Reaction Steps

1320 mg (4.7 mmol) of 7-[4-(trifluoromethyl)phenyl][1,2,4]triazolo[1,5-c]pyrimidin-5-ol (Example 138A) are introduced into phosphoryl chloride (20 ml), 3.20 g (14 mmol) of benzyltriethylammonium chloride are added, and the reaction mixture is stirred at 120° C. for 4 h. The reaction mixture is slowly poured, while stirring vigorously, into saturated sodium bicarbonate solution (150 ml) and ice, and solid sodium bicarbonate (approx. 10 g) is added until a pH of 8 is reached. The solid is filtered off with suction. 1300 mg (92% of theory) of the crude product are obtained.

Provenance & Evidence