Ammonia → 6-Phenyl-5-(4-{[4-(5-pyridin-2-yl-1H-1,2,4-triazol-3-yl)piperidin-1-yl]methyl}phenyl)[1,2,4]triazolo[1,5-a]pyrimidin-2-amine

Participants

Reaction Conditions

Reaction Steps

To 500 mg 2-bromo-6-phenyl-5-(4-{[4-(5-pyridin-2-yl-1H-1,2,4-triazol-3-yl)piperidin-1-yl]methyl}phenyl)[1,2,4]triazolo[1,5-a]pyrimidine (prepared as described under example 53) in 3 ml THF and 5 ml ethanol are added 8 ml of a ammonia solution (25% in water). The reaction mixture is heated to 140° C. for 22 hours. The solvent is evaporated and the solid residue is stirred in diethyl ether/ethanol (9:1). The product is filtrated, dried and further purified by RP HPLC (water, 10 mM NH4COOH, pH 3.7/ACN) to yield the desired compound.

Provenance & Evidence