1H-1,2,4-Triazole → N-(4-fluorobenzyl)-6-(4-fluorophenyl)-4-(1H-1,2,4-triazol-1-yl)pyrido[3,2-d]pyrimidin-2-amine

Participants

Reaction Steps

A solution of 2-(4-fluorobenzylamino)-6-(4-fluorophenyl)pyrido[3,2-d]pyrimidin-4-ol (2 g), 1,2,4-triazole (1.52 g), DIEA (3.55 g) and POCl3 (3.4 g) in acetonitrile (20 mL) was stirred at room temperature for 1 hour. Ethyl acetate was added to the mixture, which was then washed twice with brine. The organic layer was dried and concentrated to provide 2.1 g of N-(4-fluorobenzyl)-6-(4-fluorophenyl)-4-(1H-1,2,4-triazol-1-yl)pyrido[3,2-d]pyrimidin-2-amine which was characterized by its mass spectrum as follows: MS (m/z) 416 [M+H]+.

Provenance & Evidence