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

Participants

Reaction Conditions

Reaction Steps

650 mg (1.9 mmol) of 2-(trifluoromethyl)-7-[4-(trifluoromethyl)phenyl][1,2,4]triazolo[1,5-c]-pyrimidin-5-ol (Example 131A) are introduced into phosphoryl chloride (10 ml), 1.28 g (5.6 mmol) of benzyltriethylammonium chloride are added, and the reaction mixture is stirred at 120° C. for 12 h. The reaction mixture is slowly poured, with vigorous stirring, into saturated sodium bicarbonate solution (50 ml) and ice, and solid sodium bicarbonate (approx. 1 g) is added until a pH of 8 is reached. The solid is filtered off with suction. 635 mg (93% of theory) of the crude product are obtained.

Provenance & Evidence