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

Participants

Reaction Conditions

Reaction Steps

1250 mg (3.3 mmol) of 7-(2,4-dichlorophenyl)-2-(morpholin-4-ylmethyl)[1,2,4]triazolo-[1,5-c]pyrimidin-5-ol (Example 134A) are introduced into phosphoryl chloride (20 ml), 2.25 g (9.9 mmol) of benzyltriethylammonium chloride are added, and the reaction mixture is stirred at 120° C. for 12 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 and dried. 508 mg (39% of theory) of the product are obtained.

Provenance & Evidence